7621-81-0Relevant articles and documents
Design, Synthesis, and Antimicrobial Activity of Novel Fluorine-Containing Imidazolones
Desai,Wadekar,Mehta,Pandit
, p. 976 - 985 (2021/08/09)
Abstract: A simple synthetic protocol have been developed for the preparation of novelN-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydro-1H-imidazol-1-yl)-N′-phenylthiourea derivatives by the reaction of4-benzylidene-2-phenyl-4,5-dihydro-1,3-oxazol-5-ones with N
Benzothiazol clubbed imidazol-4-ones as anti-fungal, anti-tubercular and anti-HIV-1 agents: Their synthesis and molecular docking study
Patel, Navin B.,Shaikh, Asif R.,Patel, Vatsal M.,Lara-Ramirez, Edgar E.,Rivera, Gildardo
, p. 382 - 391 (2019/06/18)
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).
Silica-supported Solvent Approaches More Facile than the Conventional for Erlenmeyer Synthesis with Our Pyridinium Salts
Manikandan, Chitrarasu,Ganesan, Kilivelu
, p. 929 - 934 (2018/02/19)
The synthesis of pyridinium salts by both conventional/silica-supported muffle furnace and microwave approaches is described. We have optimized the Erlenmeyer synthesis of azalactone with various concentrations of our synthesized pyridinium salts. Among t
Sulfanilic acid-catalyzed green synthesis of 4-Arylidene-2-phenyl-5(4H)-Oxazolones
Kiyani, Hamzeh,Aslanpour, Shiva
, p. 297 - 303 (2018/02/22)
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
Synthesis of Erlenmeyer-Pl?chl azlactones promoted by 5-Sulfosalicylic acid
Kiyani, Hamzeh,Aslanpour, Shiva
, p. 1314 - 1321 (2017/07/18)
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
Greener approach: Ionic liquid [Et3NH][HSO4]-catalyzed multicomponent synthesis of 4-arylidene-2-phenyl-5(4H)oxazolones under solvent-free condition
Jadhav, Santosh A.,Sarkate, Aniket P.,Farooqui, Mazahar,Shinde, Devanand B.
, p. 1676 - 1683 (2017/09/08)
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.
Synthesis and quantitative structure-activity relationships study for phenylpropenamide derivatives as inhibitors of hepatitis B virus replication
Yang, Jing,Ma, Min,Wang, Xue-Ding,Jiang, Xing-Jun,Zhang, Yuan-Yuan,Yang, Wei-Qing,Li, Zi-Cheng,Wang, Xi-Hong,Yang, Bin,Ma, Meng-Lin
, p. 82 - 91 (2015/07/27)
A series of new phenylpropenamide derivatives containing different substituents was synthesized, characterized and evaluated for their anti-hepatitis B virus (HBV) activities. The quantitative structure eactivity relationships (QSAR) of phenylpropenamide compound have been studied. The 2D-QSAR models, based on DFT and multiple linear regression analysis methods, revealed that higher values of total energy (TE) and lower entropy (Sθ) enhanced the anti-HBV activities of the phenylpropenamide molecules. Predictive 3D-QSAR models were established using SYBYL multifit molecular alignment rule. The optimum models were all statistically significant with cross-validated and conventional coefficients, indicating that they were reliable enough for activity prediction.
One flask synthesis of esters of the corresponding 3-substituted 2-benzoylamino acrylic acids using 2-oxazolin-5-ones as synthons
Ahmed, Md. Mizanur,Borthakur, Somadrita,Tripathy, Pradeep K.
, p. 371 - 372 (2019/01/21)
A modified route for the fast and facile synthesis of an alkyl 3-substituted 2- benzoylamino acrylate (4) is hereby developed. All the required steps are carried out in the same flask.
A green protocol for Erlenmeyer-Pl?chl reaction by using iron oxide nanoparticles under ultra sonic irradiation
Ahmadi, Seyed Javad,Sadjadi, Sodeh,Hosseinpour, Morteza
, p. 408 - 412 (2013/01/15)
Azlactones have been prepared via Erlenmeyer synthesis from aromatic aldehydes and hippuric acid using Fe2O3 nanoparticles under ultrasonic irradiation. Short reaction times, easy and quick isolation of the products, and excellent yi
Ammonium metavanadate an efficient catalyst for Erlenmeyer synthesis
Madje, Balaji,Ubale, Milind,Bharad, Jagdish,Shingare, Murlidhar
, p. 1295 - 1299 (2013/01/15)
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
