- Synthesis and luminescence properties of analogues of the green fluorescent protein chromophore
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The green fluorescent protein (GFP) is extensively used as a biomarker for fluorescence biological imaging. The chromophore in GFP is only fluorescent when confined into the β–barrel of the protein. Similarly, synthetic analogues of the fluorophore of GFP
- Esteves, Cátia I. C.,Guieu, Samuel,Rocha, Jo?o,Silva, Artur M. S.,da Silva Fonseca, Inês
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- Discovery of a necroptosis inhibitor improving dopaminergic neuronal loss after mptp exposure in mice
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Parkinson’s disease (PD) is the second most common neurodegenerative disorder, mainly characterized by motor deficits correlated with progressive dopaminergic neuronal loss in the substantia nigra pars compacta (SN). Necroptosis is a caspase-independent f
- Oliveira, Sara R.,Dionísio, Pedro A.,Gaspar, Maria M.,Ferreira, Maria B. T.,Rodrigues, Catarina A. B.,Pereira, Rita G.,Estev?o, Mónica S.,Perry, Maria J.,Moreira, Rui,Afonso, Carlos A. M.,Amaral, Joana D.,Rodrigues, Cecília M. P.
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- Benzothiazol clubbed imidazol-4-ones as anti-fungal, anti-tubercular and anti-HIV-1 agents: Their synthesis and molecular docking study
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Background: The present work describes antimicrobial, antimycobacterium and anti HIV-1 evaluation of newly synthesized 5-(4-Substituted-benzylidene)-3-[4-(5-methyl-benzothiazol2-yl)-phenyl]-2-phenyl-3,5-dihydro-imidazol-4-one (4a-o). The docking studies were performed in order to predict the potential binding affinities. Objective: The major aim of this study is to develop the new class of bezylidine candidate clubbed with benzothiazole with less toxicity and improved potency as antimicrobial, antitubercular and anti HIV-1. Methods: The titled compounds were characterized by spectral studies (IR, 1H NMR, 13C NMR and Mass). In vitro antimycobacterium activity was carried out using Lowenstein-Jensen medium method and antimicrobial activity using the broth microdilution method. The anti HIV-1 reverse transcriptase activity was determined by the colorimetric MTT method and inhibition of virusinduced cytopathogenicity in MT-4 cells. Results: Compound 4i (50 μM) showed better antifungal activity against A. clavatus. Compound 4g (50 μM) with 95% inhibition demonstrated good activity against M. tuberculosis H37Rv. Compound 4k showed CC50 (50 μM) against MT-4 (CD4+ Human T-cells containing an integrated HTLV-1 genome) cells by 50%, while 16 μM concentration value EC50 from the HIV-1 induced cytopathogenicity. Molecular docking study suggested that 4k interacted with the target with binding energy by Vina score (-10.3 Kcal/mol) Conclusion: The preliminary in vitro evaluation results revealed that some of the compounds have promising antimicrobial activities as well as antitubercular potency. Among the various substituents on benzylidene, the nitro group was the most beneficial for improving the anti-HIV-1 activity. Docking result suggested that 4k compound could be acting as a non-competitive or weak inhibitor of Reverse Transcriptase (RT).
- Patel, Navin B.,Shaikh, Asif R.,Patel, Vatsal M.,Lara-Ramirez, Edgar E.,Rivera, Gildardo
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p. 382 - 391
(2019/06/18)
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- Synthesis and herbicidal activity of 4-benzylidene-2-phenyl oxazol-5(4H)-one derivatives using l-proline as catalyst
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A simple, efficient and environmentally benign method for the synthesis of 4-benzylidene-2-phenyl oxazol-5(4H)-one derivatives by the reaction of aromatic aldehydes and hippuric acid using acetic anhydride as dehydrating agent and L-proline as catalyst ha
- Bhandari,Kasana
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p. 1717 - 1722
(2018/07/10)
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- An ionic liquid gel: A heterogeneous catalyst for Erlenmeyer-Plochl and Henry reactions
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An ionic liquid gel has been prepared by entrapping 1-butyl-3-methylimidazolium hydroxide ([Bmim]OH) in an aqueous agar gel. The ionic liquid gel has been characterized by Fourier transform infrared (FT-IR), Fourier transform Raman (FT-Raman) spectroscopy, scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and energy dispersive X-ray analysis (EDX). The ionic liquid gel has been successfully employed as a heterogeneous catalyst in the Erlenmeyer-Plochl reaction involving aldehydes, hippuric acid and acetic anhydride as well as in the Henry reaction between aldehydes and nitromethane in ethanol at room temperature. The heterogeneity of the ionic liquid gel has been confirmed by conducting hot filtration tests and leaching studies. Additionally, the ionic liquid gel could be easily recovered by simple filtration and reused five times without significant loss in catalytic activity.
- Jagadale, Megha,Naikwade, Altafhusen,Salunkhe, Rajashri,Rajmane, Mohan,Rashinkar, Gajanan
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p. 10993 - 11005
(2018/07/06)
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- Sulfanilic acid-catalyzed green synthesis of 4-Arylidene-2-phenyl-5(4H)-Oxazolones
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This study is focused on the catalytic activity of sulfanilic acid (SA) in the straightforward synthesis of 4-Arylidene-2-phenyl-5(4H)-oxazolones via condensation of aromatic aldehydes, hippuric acid, and acetic anhydride under green experimental conditio
- Kiyani, Hamzeh,Aslanpour, Shiva
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p. 297 - 303
(2018/02/22)
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- Greener approach: Ionic liquid [Et3NH][HSO4]-catalyzed multicomponent synthesis of 4-arylidene-2-phenyl-5(4H)oxazolones under solvent-free condition
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We have developed simple, greener, safer multicomponent synthesis series of 4-arylidene-2-phenyl-5(4H) oxazolones 4(a-r) catalyzed by Bronsted acid ionic liquid as triethylammonium hydrogen sulfate [Et3NH][HSO4] and catalytic amount of acetic anhydride and sodium acetate with excellent yields (90–99%). The protocol offers economical, environmentally benign, solvent-free conditions, and recycle–reuse of the catalyst and easily available starting as benzoyl chloride 1, amino acid 2 and a variety of aldehydes 3. The cyclization followed by condensation of benzoyl chloride, amino acid, and a variety of aldehydes catalyzed by ILs [Et3NH][HSO4] and catalytic amount of acetic anhydride and sodium acetate. The final products were confirmed by their characterization data such as FTIR, 1H-NMR, 13C-NMR, Mass, high-resolution mass spectra and were compared with its reported method.
- Jadhav, Santosh A.,Sarkate, Aniket P.,Farooqui, Mazahar,Shinde, Devanand B.
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p. 1676 - 1683
(2017/09/08)
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- Triphenylphosphine (PPh3) Catalyzed Erlenmeyer Reaction for Azlactones under Solvent-free Conditions
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This study presents triphenylphosphine catalyzed process for the synthesis of azlactones and their derivatives using hippuric and substituted aromatic aldehydes. The methodology also found to be effective for the synthesis of azlactones from 5-(2,6-dichlorophenyl)-3-methyl-1,2-oxazol-4-yl carbonyl amino acetic acid and offers several advantages such as solvent-free conditions, excellent yields, simple procedure, mild conditions, and reduced environmental consequences.
- Punna Rao, Alapati Mohan Lakshmi,Sridhar Rao, Abburi,Saratchandra Babu, Mukkamala,Krishnaji Rao
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supporting information
p. 429 - 435
(2017/02/03)
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- Synthesis of Erlenmeyer-Pl?chl azlactones promoted by 5-Sulfosalicylic acid
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5-Sulfosalicylic acid was found as an efficient catalyst in the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones by condensation and cyclodehydration of aromatic aldehydes with hippuric acid and acetic anhydride at room temperature. The catalyst was eas
- Kiyani, Hamzeh,Aslanpour, Shiva
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p. 1314 - 1321
(2017/07/18)
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- Microwave-assisted efficient synthesis of azlactones using zeolite NaY as a reusable heterogeneous catalyst
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The efficient preparation of azlactones in the presence of zeolite NaY has been reported. This heterogeneous catalyst was used for efficient synthesis of azlactone derivatives with Ac2O as a condensing agent under microwave irradiation and solvent-free co
- Bodaghifard, Mohammad Ali,Moghanian, Hassan,Mobinikhaledi, Akbar,Esmaeilzadeh, Fatemeh
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p. 845 - 849
(2017/08/10)
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- A Facile and Efficient Synthesis of 4-Arylidene-2-phenyl-5(4H)-oxazolones and Their Antimicrobial Evaluation against Selected Human and Phytopathogens
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A simple and convenient method has been developed for the synthesis of a series of 2-(4-substituted phenyl)-4-(substituted arylidene)-1,3-oxazol-5-ones (5a–j) via reactions of hippuric acid with differently substituted aromatic aldehydes (4a–j) in sodium acetate, potassium acetate, calcium acetate, and ammonium acetate, respectively, which were tested for their efficiency as catalysts in both conventional and microwave-assisted synthetic methods in presence of 4 ? zeolites. The title compounds were evaluated for their antimicrobial properties against selected human pathogens (bacterial and fungal) and phytopathogens (fungal) and were compared with standard drugs. The results of the study are reported.
- Voosala, Christopher,Kilaru, Padma Suhasini,Dasari, Uday Kumar
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p. 909 - 916
(2016/11/23)
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- Synthesis of 4-(thiazol-2-ylamino)-benzenesulfonamides with carbonic anhydrase I, II and IX inhibitory activity and cytotoxic effects against breast cancer cell lines
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A series of 4-(thiazol-2-ylamino)-benzenesulfonamides was synthesized and screened for their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory and cytotoxic activity on human breast cancer cell line MCF-7. Human (h) CA isoforms I, II and IX were included in the study. The new sulfonamides showed excellent inhibition of all three isoforms, with KIs in the range of 0.84-702 nM against hCA I, of 0.41-288 nM against hCA II and of 5.6-29.2 against the tumor-associated hCA IX, a validated anti-tumor target, with a sulfonamide (SLC-0111) in Phase I clinical trials for the treatment of hypoxic, metastatic solid tumors overexpressing CA IX. The new compounds showed micromolar inhibition of growth efficacy against breast cancer MCF-7 cell lines.
- Abdel Gawad, Nagwa M.,Amin, Noha H.,Elsaadi, Mohammed T.,Mohamed, Fatma M.M.,Angeli, Andrea,De Luca, Viviana,Capasso, Clemente,Supuran, Claudiu T.
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p. 3043 - 3051
(2016/06/13)
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- An innovation for development of Erlenmeyer-Pl?chl reaction and synthesis of AT-130 analogous: A new application of continuous-flow method
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The development of eco-friendly and efficient processes via one-pot multicomponent synthesis is a very attractive topic. In this work, the Erlenmeyer-Pl?chl azlactone synthesis was carried out through unique, safe, fast and practical conditions without any catalyst, applying a simple microreactor and gave the corresponding products exclusively. A continuous, first microflow synthesis of N-benzoylglycine carbamide derivatives as AT-130 analogues catalyzed by Nafion-H@SPIONs was also established successfully.
- Shafiee, Behnaz,Hadian, Laleh,Khosropour, Ahmad R.
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p. 19861 - 19866
(2016/03/04)
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- Microwave-Assisted Erlenmeyer Synthesis of Azlactones Catalyzed by MgO/Al2O3 under Solvent-Free Conditions
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MgO/Al2O3 catalyzes the synthesis of azlactone derivatives from condensation reaction of aldehydes (or ketones) with hippuric acid and acetic anhydride as a dehydrating agent under microwave irradiation. The low toxicity, low cost, ease of handling, and high activity of MgO/Al2O3 make this procedure particularly attractive. Also, this catalyst can be easily recovered by decant and can be reused for this condensation five times in succession without considerable loss of its catalytic activity.
- Rostamizadeh, Nader,Khajeh-Amiri, Alireza,Moghanian, Hassan
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p. 631 - 634
(2015/12/26)
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- Microwave-assisted efficient and mild synthesis of azlactone derivatives
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(Formula presented) A convenient and mild procedure for the synthesis of azlactones in the presence of catalytic amounts of calcium hydrogen phosphate as a green, inexpensive and environmentally benign catalyst has been demonstrated. The present protocol is operationally simple and offers some advantages such as good yields, short reaction time, simple work-up, low cost and reusability of catalyst, which makes this method mild and eco-friendly.
- Bodaghifard, Mohammad Ali,Mobinikhaledi, Akbar,Moradi, Khosro
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p. 193 - 197
(2016/07/15)
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- A convenient synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones under solvent-assisted grinding
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A facile and effective approach for the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones has been developed. Under solvent-assisted grinding in the presence of 2,4,6-trichloro-1,3,5-triazine, catalytic triphenylphosphine, and sodium carbonate, dehydrati
- Pattarawarapan, Mookda,Jaita, Subin,Phakhodee, Wong
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supporting information
p. 3171 - 3174
(2016/07/06)
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- Synthesis and characterization of novel chalcone linked imidazolones as potential antimicrobial and antioxidant agents
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A series of ten 4-(4-(dimethylamino)benzylidene)-1-(4-(3-(aryl)acryloyl) phenyl)-2-phenyl-1H-imidazol-5(4H)-ones (7) have been synthesized by condensation of 1-(4-acetylphenyl)-4-(4-(dimethylamino)benzylidene)-2-phenyl-1H-imidazol-5(4H)-one (5) with different aryl aldehydes (6). The structures of the newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR, Mass spectral studies and elemental analysis. All the above compounds were screened for their antimicrobial activity against gram positive bacteria B. subtilis, S. aureus, gram negative bacteria E. coli, P. vulgaris and the yeast C. albicans. These compounds were also tested for antioxidant activity by DPPH method and were found to be biologically active.
- Sadula, Anitha,Peddaboina, Usha Rani,Prameela Subhashini
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p. 851 - 859
(2015/01/30)
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- Synthesis of Erlenmeyer azlactones using arylsulphonyl chloride as cyclocondensing agent
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A fast and facile procedure for one flask synthesis of (Z)-2-substituted-4- arylmethylene-2-oxazolin-5-ones (3) which are popularly known as Erlenmeyer azlactones, is being reported starting from N-acylglycines (1) and different aromatic aldehydes using arylsulphonyl chloride as cyclocondensing agent in the presence of triethyl amine base and dry benzene. The reaction time is reduced to minute under milder conditions alongwith higher yields of the products.
- Goswami, Limi,Tripathy, Pradeep K.
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p. 281 - 282
(2019/01/21)
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- [Et3NH][HSO4]-mediated functionalization of hippuric acid: an unprecedented approach to 4-arylidene-2-phenyl-5(4H)-oxazolones
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A facile, green and stereoselective approach for the synthesis of azlactones/oxazolones 3(a-q) has been developed. The protocol involves reaction of hippuric acid and substituted heterocyclic/aromatic aldehydes in ionic liquid [Et3NH][HSO4] to yield the desired 4-arylidene-2-phenyl-5(4H)-oxazolones in excellent yields (94-97%) with a high degree of purity. The remarkable feature of this pathway is that the ionic liquid eliminates the use of toxic and expensive acetic anhydride and is endowed with catalytic and medium engineering ability. This eco-friendly approach improved synthetic efficiency (94-97% yield), minimizing the production of chemical waste without using highly toxic reagents for the synthesis and more notably, it promoted the selectivity for Z-azlactones/oxazolones. Density functional theory (DFT) calculations revealed that the Z-isomer of compound 3a is stabilised by 2.32 kcal mol-1 more than the E-isomer. This synthetic scheme possesses diverse applicability and is compatible to a range of functional groups (electron donating/electron withdrawing).
- Parveen, Mehtab,Ahmad, Faheem,Malla, Ali Mohammed,Azaz, Shaista,Silva, Manuela Ramos,Silva, P. S. Pereira
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p. 52330 - 52346
(2015/06/25)
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- Synthesis, in-vitroreverse transcriptase inhibitory activity and docking study of some new imidazol-5-one analogs
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Non-nucleoside reverse transcriptase inhibitors have a definitive role and most commonly used in treatment of HIV-1 infection. A new series of 4-ethylidene/substituted-benzylidene-1-(4-hydroxy/chloro-6-methylpyrimidin-2-yl) -2-ethyl/phenyl-1H-imidazol-5(4H)-one were designed, synthesized, and evaluated for HIV-1 reverse transcriptase (RT) inhibitory activity. The results of in-vitro HIV-1 RT assay showed that some of the new compounds, such as 4c, 4d, 4e, 5a, and 5e effectively inhibit HIV-1 RT activity. 1-(4-Chloro-6- methylpyrimidin-2-yl)-4-(furan-2-ylmethylene)-2-methyl-1H-imidazol-5(4H)-one (5e) exerted most potent in-vitro HIV-1 RT inhibitory activity, among the group of compounds. Molecular docking studies were carried out to explore the binding affinity of imidazole-5-one analogs in active site of HIV-1 RT enzyme. Springer Science+Business Media 2014.
- Mokale, Santosh N.,Lokwani, Deepak K.,Shinde, Devanand B.
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p. 3752 - 3764
(2014/08/05)
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- Efficient synthesis of 5(4H)-imidazolones and IN VITRO antifungal activity studies against selected phytopathogens
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A series of five new 1-(substituted phenyl)-2-phenyl-4-(substituted benzylidine)imidazole-5-one derivatives (or) 5(4H)-imidazolones I have been synthesized adopting SiO2, Al2O3-90 and Y-faujasite (Y-H type) zeolite as cata
- Voosala, Christopher,Yellajyosula, Lakshmi Narasimha Murthy,Uppuleti, Viplava Prasad,Kilaru, Padma Suhasini
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p. 2873 - 2876
(2014/06/09)
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- Synthesis, characterization and anticonvulsant activity of substituted imidazolinone derivatives
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The reaction of glycine with benzoylchloride gave 2-benzamidoacetic acid (1) which on reaction with substituted benzaldehydes in presence of acetic anhydride and anhydrous sodium acetate gave 4-benzylidene-2-phenyloxazol-5(4H)-one derivatives (2a-h). 4-Ni
- Sudha, B. Naga,Subbaiah, N. Yella,Raghavendra,Srikanth,Reddy, C.Venkataramana,Manasa
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p. 159 - 162
(2019/01/21)
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- In vitro antitubercular, antibacterial and antifungal activities of 4- (3,4-disubstituted) benzylidene -2- phenyloxazolin-5-ones and their phenyl acrylohydrazides
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Some new 2-benzamido-3-(3,4-substituted) phenylacrylohydrazides 3a-g were synthesized from 4-(3,4-substituted) benzylidene-2-phenyl oxazol-5(4H)-ones 2a-g and characterized by IR, 1H NMR, 13C NMR and mass spectral and elemental analy
- Ramalingam,Ramakanath Reddy,Babu Rao, Ch.,Hari Babu,Vasudev
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p. 321 - 330
(2019/01/21)
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- Sonochemical hot-spot assisted one-pot synthesis of 4-arylmethylidene-2- phenyl-4H-oxazol-5-ones using nano-mgo as an efficient catalyst
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Twelve 4-arylmethylidene-2-phenyl-4H-oxazol-5-ones were prepared in excellent yield by sonicating a mixture of an araldehyde, hippuric acid and acetic anhydride in the presence of a green heterogeneous NanoMgO as a basic catalyst. The catalytic activity o
- Saleh Azzam, Sadeq Hamood,Chandrappa,Pasha, Mohamed Afzal
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p. 283 - 290
(2013/07/26)
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- In viro antitubercular, antibacterial and antifungal activities of 4- (3,4-disubstituted) benzylidene-2-phenyloxazolin-5-ones and their phenyl acrylohydrazides
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Some new 2-benzamido -3-(3,4-substituted) phenylacrylohydrazides 3a-g were synthesized from 4-(3,4-substituted) benzylidene-2-phenyl oxazol-5-(4H)-ones 2a-g and characterized by IR, 1H NMR, 13C-NMR and mass spectral studies. Compound
- Ramalingam,Padmanabha Reddy,Ramakanth Reddy,Hari Babu,Vasudev
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p. 165 - 170
(2019/01/21)
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- Synthesis, biological activity and docking study of imidazol-5-one as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
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A novel series of substituted imidazol-5-ones were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) inhibition activity using reverse transcriptase assay kit (Roche, Colorimetric). It has been observed from in vitro screening that newly synthesized compounds possess RT inhibitory activity. Docking study was performed to study the binding orientation and affinity of synthesized compounds for RT enzyme.
- Mokale, Santosh N.,Lokwani, Deepak,Shinde, Devanand B.
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p. 3119 - 3127
(2012/06/29)
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- Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity
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A series of substituted (benzamidostyryl) benzimidazole (3a-r) were synthesized and evaluated for their possible anti-inflammatory and ulcerogenicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Majority of the compounds were active in carrageenaninduced hind paw edema method test and compounds 3b, 3k had shown high potency after 3 and 4 h time intervals (P0.001) almost equipotent to the standard drug indomethacin and showed less severity index than it. Springer Science+Business Media, LLC 2011.
- Kaushik, Darpan,Khan, Suroor Ahmed,Chawla, Gita
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p. 459 - 467
(2012/08/07)
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- Synthesis and antimicrobial screening of N-[2-(2/4-substituted phenyl)-1-(5/6 substituted 1H- benzimidazol-2-yl)vinyl]benzamides
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A series of (benzamidostyryl)benzimidazole derivatives were synthesized by hydrolyzing 2-phenyl-4-(substituted)benzylidene-5-oxazolones, the azlactone precursors in an acidic medium and treating the product with substituted o-phenylenediamine (OPDA) in si
- Kaushik, Darpan,Khan, Suroor A.,Chawla, Gita,Panda, Bibhu P.
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body text
p. 629 - 636
(2012/08/29)
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- Microwave-assisted efficient synthesis of azlactone derivatives using TsCl/DMF under solvent-free conditions
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A simple and efficient procedure for the synthesis of azlactones employing condensation reaction of aromatic aldehydes with hippuric acid has been developed by using the tosyl chloride (TsCl) and dimethylformamide (DMF) system as condensing agent in the absence of solvents under microwave irradiation. The present protocol is operationally simple and offers several advantages such as high yields, short reaction time, and simple workup.
- Moghanian, Hassan,Shabanian, Meisam,Jafari, Hadi
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experimental part
p. 346 - 349
(2012/06/30)
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- Ammonium metavanadate an efficient catalyst for Erlenmeyer synthesis
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An efficient method to synthesize azalactone derivatives using ammonium metavanadate (NH4VO3) as catalyst was performed in the absence of solvent. This method is environmentally friendly and affords the product azalactones in high yi
- Madje, Balaji,Ubale, Milind,Bharad, Jagdish,Shingare, Murlidhar
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p. 1295 - 1299
(2013/01/15)
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- Facile synthesis of 4-arylidene-5-imidazolinones as synthetic analogs of fluorescent protein chromophore
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A facile and effective synthesis for a wide variety of 4-arylidene-5- imidazolinone derivatives was developed. 4-Arylidene-5-oxazolinones were prepared by Erlenmeyer azlactone synthesis from N-acylglycines and arylaldehydes. The ring-opening reactions of the 4-arylidene-5-oxazolinones with primary amines afforded 2-acylamino-3-arylacrylamides in excellent yields. A new dehydrative cyclization of the 2-acylamino-3-arylacrylamides in pyridine under reflux furnished the corresponding 4-arylidene-5-imidazolinones in good yields.
- Lee, Cheng-Yu,Chen, Yun-Chung,Lin, Hao-Chun,Jhong, Yuandong,Chang, Chih-Wei,Tsai, Ching-Hua,Kao, Chai-Lin,Chien, Tun-Cheng
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supporting information; experimental part
p. 5898 - 5907
(2012/09/07)
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- Synthesis, in silico metabolic and toxicity prediction of some novel imidazolinones derivatives as potent anticonvulsant agents
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A series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetate and acetic anhydride. The derivatives of the compounds we
- Hari Narayana Moorthy,Saxena, Vipin,Karthikeyan,Trivedi, Piyush
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experimental part
p. 201 - 207
(2012/07/13)
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- Two-photon absorption properties of push-pull oxazolones derivatives
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New fluorescent oxazolone derivatives with high two-photon absorption cross-section were synthesized. Electron donor (phenyl, dimethylaniline and furanyl) and acceptor (nitrobenzene and ethenyl-phenyl-benzimidazol) groups have been appended to the methyle
- Rodrigues, Catarina A.B.,Mariz, Inês F.A.,Ma??as, Ermelinda M.S.,Afonso, Carlos A.M.,Martinho, José M.G.
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p. 713 - 722
(2012/11/06)
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- 2W10O32. 2H2O: A novel and powerful catalyst for the synthesis of 4-arylidene-2-phenyl-5(4)-oxazolones under ultrasonic condition
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Di[1,6-bis(3-methylimidazolium-1-yl)hexane] decatungstate dihydrate ([C6(MIm)2]2W10O32. 2H2O) as a new family of polyoxometalate-based dicationic ionic liquids (POM-DIL) is synthesized and employed as a novel and powerful heterogeneous catalyst in the synthesis of 4-arylidene-2-phenyl-5(4)-oxazolones (azlactones) under ultrasound-assisted solvent-free condition. On the basis of the results, the products were obtained in excellent yields under mild condition. Utilization of easy work-up and purification make it very interesting from an economic perspective. Moreover, a recycling study confirmed that the catalyst can be reused multiple times without significant loss of its activity.
- Rostami, Mahboubeh,Khosropour, Ahmad R.,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Moghadam, Majid,Tangestaninejad, Shahram
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experimental part
p. 869 - 877
(2012/04/23)
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- Aminocarbonyl arylvinylbenzamides as gastric sparing anti-inflammatory agents
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Some (E/Z)-aminocarbonyl arylvinylbenzamides (B1-B15) were synthesized, evaluated for anti-inflammatory activity and ulcerogenic tendency, and their effect on gastro-intestinal motility in the rats was studied. These benzamides comprising of aliphatic unsaturated region situated between two amide linkages were synthesized by nucleophilic ring opening of appropriate azlactones (AZ1-AZ4) by suitable amines. The characterization of newly synthesized benzamides was performed by IR, 1H- and 13C-NMR, mass and elemental analysis. Amongst the tested compounds, benzamide B1, B2, B4, B5, and B13 were able to produce comparable or superior anti-inflammatory activity at 10 and 20 mg/kg p.o. dose with respect to standard diclofenac in carrageenan induced rat paw edema model with lessened propensity to cause gastro-intestinal hypermotility and were found to have nil tendencies to generate gastric ulcers. A series of N-[(E/Z)-2-(4-substituted/unsubstitutedphenyl)-1-{[arylamino] carbonyl} vinyl]benzamides (B1-B15) was synthesized by utilizing easily accessible starting material 4-substituted/unsubstituted benzylidene-2- phenyloxazol-5-one (AZ1-AZ4) and subjected to anti-inflammatory activity, gastrointestinal motility, and gastric damage studies in rats. Copyright
- Khadse, Saurabh C.,Talele, Gokul S.,Agrawal, Surendra S.
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scheme or table
p. 292 - 300
(2011/11/05)
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- Organic-inorganic hybrid polyoxometalates: Efficient, heterogeneous and reusable catalysts for solvent-free synthesis of azlactones
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Two organic-inorganic hybrid polyoxometalates, consist of 1-butyl-3-methylimidazolium salts of (W10O32)4- and (PW12O40)3- polyanions were prepared and characterized by thermal analysis, X-ray diffraction, FT-IR, diffuse reflectance UV-Vis spectroscopic methods and nitrogen absorption-desorption determination (BET). These heterogeneous catalysts were used for synthesis of azlactones by the reaction of aldehydes with hippuric acid and acetic anhydride under solvent-free conditions. These catalysts were reused several times without loss of their activities.
- Rostami, Mahbubeh,Khosropour, Ahmadreza,Mirkhani, Valiollah,Moghadam, Majid,Tangestaninejad, Shahram,Mohammadpoor-Baltork, Iraj
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experimental part
p. 27 - 34
(2012/01/03)
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- Synthesis and electronic spectra of new low-molecular weight compounds with possible application in electroluminescent layers
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Two new low-molecular weight compounds - (Z)-4-(4-(dimethylamino) benzylidene)-1-(9-ethyl-9H-carbazol-3-yl)-2-phenyl-1Himidazol- 5(4H)-one and 2-(6-hydroxyhexyl)-6-(pyrrolidin-1-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione) - with possible application in or
- Dobrikov, Georgi H.,Dobrikov, Georgi M.,Aleksandrova, Mariya
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experimental part
p. 1126 - 1132
(2012/04/10)
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- One-pot process to Z-α-benzoylamino-acrylic acid methyl esters via potassium phosphate-catalyzed Erlenmeyer reaction
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A practical and efficient two reaction sequence one-pot process for the synthesis of Z-α-benzoylamino-acrylic acid methyl esters was developed. The process involves a potassium phosphate-catalyzed Erlenmeyer reaction of aromatic aldehydes with hippuric acid followed by an oxazolone ring-opening methanolysis. This process afforded a good overall yield and an excellent product quality via a simple workup.
- Cleary, Thomas,Brice, Jodie,Kennedy, Nicole,Chavez, Flavio
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supporting information; experimental part
p. 625 - 628
(2010/04/05)
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- Synthesis and antimicrobial activity of some 2-phenyl-1-[4-phenyl-1,3- thiazol-2-yl]-4-(substituted benzylidene)- imidazoline-5-ones
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A series of thiazolyl imidazolinones have been synthesized and screened for their antimicrobial activity. Few of the compounds have shown promising activity against Gram positive organisms when compared with the standard drug.
- Rao, Gopal Krishna,Rajasekaran,Pai, P. N. Sanjay,Murthy, M. Srinivasa,Sengupta, Joydeep,Devi, Kalpana
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experimental part
p. 303 - 304
(2011/12/15)
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- Synthesis and pro-kinetic activity of novel substituted aminocarbonyl arylvinylbenzamides
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Synthesis of benzamides (B1-B8) and their effect on gastrointestinal motility (prokinetic activity) in the rats is being reported in this paper. The compounds were characterized by spectral analysis (IR, NMR & Mass).
- Khadse,Talele,Agarwal
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scheme or table
p. 277 - 280
(2011/12/14)
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- Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents
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A series of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2, 5-dihydro-1H-[1,2,4] triazin-6-one were designed & synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity. Among the compound tested, 5 eIX showed protection from seizures in both the animal models at dose level of 30 mg/kg while 5 bII & 5 cII showed protection against scPTZ model at same dose level. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to clinically effective drug. A series of substituted [1,2,4] triazin-6-one derivatives were synthesized, evaluated for their anticonvulsant potency on two animal models along with CNS activity and neurotoxicity and also subjected to computational parameter.
- Kaushik, Darpan,Khan, Suroor Ahmad,Chawla, Gita
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experimental part
p. 3960 - 3969
(2010/09/11)
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- Synthesis and evaluation of substituted cinnamoyl alanines for antiinflammatory, analgesic and antioxidant activities
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A series of substituted cinnamoyl alanines were synthesized by condensation of substituted 4-benzylidene-2-phenyloxazol-5-ones with alanine. The chemical structures of synthesized compounds were confirmed by means of IR, 1H NMR, mass spectral and elementa
- Rajitha,Prasad,Bharathi
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scheme or table
p. 1197 - 1204
(2012/03/11)
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- Synthesis and evaluation of substituted imidazolones for antiinflammatory and antioxidant activities
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A series of 4-substituted benzylidene-2-phenyl-1-substituted phenyl-1H-imidazol-5(4H)-one were synthesized by condensation of substituted oxazolones with p-amino benzoic acid and benzocaine. The chemical structures of synthesized compounds were confirmed
- Sarala Devi,Rajitha,Bharathi
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scheme or table
p. 5271 - 5276
(2012/07/28)
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- Tuning the excited-state dynamics of GFP-inspired imidazolone derivatives
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The excited-state dynamics of five derivatives of the GFP-chromophore, which differ by the position and nature of their substituents, has been investigated in solvents of various viscosity and polarity and in rigid media using femtosecond-resolved spectro
- Petkova, Irina,Dobrikov, Georgi,Banerji, Natalie,Duvanel, Guillaume,Perez, Robert,Dimitrov, Vladimir,Nikolov, Peter,Vauthey, Eric
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experimental part
p. 10 - 20
(2010/05/11)
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- A new, efficient and chemoselective one-pot protocol for synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones from aryl aldehyde bisulfite adducts promoted by POCl3
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(Chemical Equation Presented) A one-pot procedure for the synthesis of 4-arylidene-2-phenyl-5(4H)oxazolones directly from aryl aldehyde bisulfite adducts in the absence of Ac2O in good to excellent yields using phosphoryl chloride is reported. In addition, the observed chemoselectivity can be considered as a noteworthy advantage of this method.
- Khosropour, Ahmad R.,Khodaei, Mohammad M.,Hoseini Jomor, Seyed J.
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p. 683 - 686
(2008/09/21)
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- Dodecatungstophosphoric acid (H3PW12O40), samarium and ruthenium (III) chloride catalyzed synthesis of unsaturated 2-phenyl-5(4H)-oxazolone derivatives under solvent-free conditions
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We have found that dodecatungstophosphoric acid (H3PW 12O40), samarium or ruthenium(III) chloride act as efficient catalysts for the synthesis of unsaturated 2-phenyl-5(4H)oxazolone derivatives under solvent-free condition
- Tikdari, Ahmad Momeni,Fozooni, Samieh,Hamidian, Hooshang
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experimental part
p. 3246 - 3252
(2009/04/10)
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- Practical preparation of Z-α-(N-acetylamino)- and Z-α-(N-benzoylamino)-α,β-unsaturated acids
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An efficient two-step synthetic procedure for the preparation of numerous variations of N-protected α,β-unsaturated α-amino acids and their corresponding esters from N-protected glycine and either aliphatic or aromatic aldehydes was developed. The reaction involved cyclization of the N-protected glycine into oxazolone, condensation with the aldehyde, and ring opening with a base. Copyright Taylor & Francis Group, LLC.
- Jursic, Branko S.,Sagiraju, Sarada,Ancalade, Dustin K.,Clark, Traneil,Stevens, Edwin D.
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p. 1709 - 1714
(2008/02/01)
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- Synthesis of some novel imidazolinones
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Imidazolinone derivatives of 4a-1 have been prepared by the condensation of known heterocyclic drug derivative with 5-oxazolone derivatives, which were prepared by Erlenmeyer condensation of benzoyl glycine with different aldehydes in the presence of sodium acetate and acetic anhydride. The compounds 3a-1 were further reacted with 5H-dibenzo (b,f) azepine -5-acid hydrazide 2 to give 4a-1 in basic condition. The constitution of the products has been supported by IR, 1H-NMR, Mass spectra and elemental analysis data.
- Bhatt, Pralav V.,Wadia, Devang N.,Patel, Rajni M.,Patel, Pravin M.
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- Montmorillonite K-10 mediated Erlenmeyer synthesis of 4-arylmethylene-2- phenyl-5(4H)-oxazolones
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Aromatic aldehydes and hippuric acid in acetic anhydride undergoes classical Erlenmeyer synthesis in the presence of a catalytic amount of Montmorillonite K-10 to afford the corresponding azlactones in excellent yields with high selectivity. The azlactone
- Karade,Shirodkar,Dhoot,Waghmare
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- Synthesis and antibacterial activity of some imidazole-5-(4H)one derivatives
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In the present study, several substituted oxazolones were synthesized by condensation of benzoylglycine with different aldehydes. From such oxazolones, substituted imidazolones were synthesized by condensation with ethylenediamine, urea and 4-N,N-dimethyl
- Saravanan, Sampath,Selvan, Perumal Senthamil,Gopal, Natesan,Gupta, Jayanta Kumar,De, Biplap
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p. 488 - 492
(2007/10/03)
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