- New thiazolyl-pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents
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A new series of N-substituted pyrazoline derivatives 6a–g, 7a–g, 8a–g, and 9a–g was synthetized by reaction of hydrazine derivatives and chalcone–thiazole hybrids bearing nitrogen mustard 5a–g. The chalcones 5a–g were obtained by Claisen–Schmidt condensation of thiazole-2-nitrogen mustard 3 and selected acetophenones 4a–g. These new compounds 6/7/8/9a–g were screened for their antifungal activity against Cryptococcus neoformans, with IC50 values of 3.9–7.8 μg/ml for the N-3,5-dichlorophenyl pyrazolines 9e–g. Interestingly, those compounds show low cytotoxic effects toward erythrocytes (RBC). In addition, N-acetyl (6a,b) and N-formyl pyrazolines (7a, 7b, 7c, and 7g) showed inhibitory activity against methicillin-susceptible Staphylococcus aureus, methicillin-resistant S. aureus, and vancomycin-intermediate S. aureus, with the most important minimum inhibitory concentration values ranging from 31.25 to 125 μg/ml. Regarding the antiprotozoal activity, thiazolyl-pyrazolines 9g, 8f, and 7c display high activity against Plasmodium falciparum, Leishmania (V) panamensis, and Trypanosoma cruzi, with EC50 values of 11.80, 6.46, and 4.98 μM, respectively, and with 7c being approximately 2.6-fold more potent than benznidazole with a selectivity index of 1.61 on U-937 human cells, showing promising potential as a novel antitrypanosomal agent.
- Cobo, Justo,Crespo, María del Pilar,Cuartas, Viviana,Insuasty, Braulio,Nogueras, Manuel,Pineda, Tatiana,Robledo, Sara M.,Sortino, Maximiliano,Upegui, Yulieth,Vélez, Iván D.,Yepes, Lina,Zacchino, Susana
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- Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
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In recent years, ALR2 (aldose reductase) inhibitors have attracted attention for their effective ability to reduce the progression of diabetes-associated cataracts. Therefore, in the present article, we intended to develop novel thiazole-sulfonamide hybrids as a potent inhibitor of ALR2. These molecules significantly inhibited the ALR2 level in the rat lenses homogenate, where the most potent compound 7b showed activity comparable to sorbinil as standard. In Wistar rats, compound 7b improved the insulin level and body weight of the experimental animal together with a reduction in the glucose output. Compound 7b showed a significant reduction in the expression of ALR2 in rat lenses in western blot analysis.
- Yin, Liang,Zhang, Mingxue,He, Tiangeng
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- Ultrasound promoted montmorillonite K-10 catalyzed synthesis, characterization, molecular modelling, SAR and hypoglycemic studies of new rhodanine bejeweled acridine analogues
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In the present work an efficient ultrasound promoted synthesis of (Z)-2-((4-chloro-2-(piperidin/morpholin-1-yl)thiazol-5-yl)methylene)-3,3,7,9 tetra methyl-3,4-dihydroacridin-1 (2H) -one analogues 6(a-h) via Knoevenagel condensation using MK-10 catalyst have been reported. MK-10 due to its diverse properties and high surface area to volume ratio exhibits favorable features for the reaction response such as the shorter reaction time, simple work-up procedure, clean reaction profiles and excellent product yields through reusability of the catalyst upto five cycles. In silico molecular docking studies were carried out to find out the effective binding affinity of the synthesized acridine analogues towards PPARγ protein (Id-2XKW). The results obtained showed that compounds 6c and 6g possess good binding interaction towards PPARγ with binding energy of -9.6 and -9.0 k.cal/mol which was greater than standard Acarbose (-8.9 k.cal/mol) and comparable to that of standard pioglitazone (-9.8 k.cal/mol). In vitro α-amylase and α-glucosidase assays were performed for hypoglycemic activity evaluation. The compounds 6c and 6g at a concentration of 100 μg/mL showed 87.18 ± 0.90 and 83.34 ± 0.15 percent inhibition towards α-glucosidase, 85.24 ± 1.06 and 80.76 ± 0.55 percent inhibition towards α-amylase which was higher than standard pioglitazone and on par to that of Acarbose.
- Angajala, Gangadhara,Aruna, Valmiki,Pavan, Pasupala,Reddy, Pulikanti Guruprasad
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- Pyrimidine-thiazolidinone derivatives
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Pyrimidine-thiazolidinone derivatives may be used for preventing or treating diseases in humans or animals, and have demonstrated efficacy specifically in treating type-2 diabetes. Methods of synthesizing the pyrimidine-thiazolidinone derivatives, described herein, can provide high yields in a short time and with high purity. The pyrimidine-thiazolidinone derivatives demonstrate improved hypoglycemic activity compared to most anti-diabetic drugs currently available.
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Page/Page column 8; 3
(2020/07/09)
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- Synthesis of carboxamide and sulfonyl carboxamide linked heterocycles under green conditions
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Direct coupling of heteroaldehydes with heteroaryl amines / sulfonylamines is performed under green conditions using PEG-400 in the presence of oxidant CCl3CN/H2O2. The presence of electron withdrawing substituents on heteroaldehydes increased the yield. Further heteroaryl amines favor the reaction when compared with heteroaryl sulfonylamines.
- Gaddam, Lakshmi Teja,Thata, Sreenivasulu,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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- Solvent-free synthesis of bis-hydrazones through 1,3-dipolar cycloaddition of sydnone and study of their optical, molecular docking, and antioxidant properties
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A series of new 1-(aryl)-1H-pyrazol-3,4-bis (aryl)-3,4-dicarbohydrazones (4) was obtained by the condensation of 1-arylpyrazole-3,4-dicarbohydrazides (3) with various aryl aldehydes under solvent-free conditions. The structures of the newly synthesized hy
- Asma,Kalluraya, Balakrishna,Manju,Adhikari,Chandra,Mahendra
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p. 335 - 344
(2018/09/29)
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- Synthesis, characterization and antioxidant property of novel series of thiazole based chalcones carrying thiophene/furan derivatives
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Two novel series of thiazole based chalcones bearing thiophene or furan derivatives (4a-h and 5a-f) were synthesized by acid/base catalyzed Claisen Schimidt condensation reaction between thiazole carbaldehyde (2) with various substituted acetylfuran (3a) or acetylthiophene (3b). The structures of these newly synthesized compounds were confirmed by their 1H-NMR, IR, Mass spectral and elemental analytical data. All the new compounds were screened for their antioxidant activity.
- Nkurunziza, Jean Baptiste,Kalluraya, Balakrishna
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- THIAZOLE DERIVATIVES FOR THE TREATMENT OF ANIMAL TRYPANOSOMIASIS
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The present invention relates to a novel class of compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein, to their use in human and veterinary medicine, and in the treatment of animal trypanosomiasis in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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Page/Page column 92; 93
(2016/10/04)
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000270
(2015/10/05)
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- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
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Paragraph 1306; 1307
(2014/07/23)
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- Synthesis and antidiabetic activity of morpholinothiazolyl-2,4- thiazolidindione derivatives
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We report the synthesis and the in vitro insulin releasing and glucose uptake activity of the morpholino thiazolyl-2,4-thiazolidinediones (1-15). Compounds 5, 1115 (at lower concentration; 0.001mg/ml) were able to increase insulin release in the presence
- Ezer, Melis,Yildirim, Leyla Tatar,Bayro, Ornela,Verspohl, Eugen J.,Dundar, Oya Bozdag
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scheme or table
p. 419 - 427
(2012/08/28)
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- N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
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The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
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Page/Page column 78
(2010/12/29)
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- Thiazole analogs of chalcones, capable of functionalization at the heterocyclic nucleus
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The synthesis of new amino and alkoxy derivatives of thiazole-5- carbaldehyde, on the basis of which a,β-unsaturated ketones of the thiazole series were synthesized, are described in this paper. The possibility of obtaining chalcones and variation of substitution reactions in the thiazole ring has been shown. 2010 Springer Science+Business Media, Inc.
- Kotlyar,Pushkarev,Orlov,Chernenko,Desenko
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experimental part
p. 334 - 341
(2011/04/22)
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- Novel chemical compounds
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This invention relates to newly identified compounds for inhibiting hYAK3 and/or CK2 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 and/or CK2 proteins.
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Page/Page column 8
(2009/10/31)
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- Synthesis and antimicrobial activity of some novel thiazolidine-2,4-dione derivatives
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In this study, a series of phenylethylsulfanyl-1,3-thiazolo-thiazolidine-2, 4-dione derivatives (VII a - f, VIIIa - f) and 5-methyl-[1,2,4]triazolyl- sulfanyl-1,3-thiazolo-thiazolidine-2,4-dione derivatives (IX a - f, Xa - f) were synthesized and evaluated for their antibacterial and antifungal activities against S. aureus (ATCC 25923), methicillin resistant S. aureus (MRSA ATCC 43300), B. subtilis (ATCC 6633), E. coli ( ATCC 23556) and C. albicans (ATCC10145). All the compounds were found active against used bacteria. ECV Editio Cantor Verlag.
- Mentese, Arzu,Ceylan-Uenluesoy, Meltem,Bozdag-Duendar, Oya,Altanlar, Nurten,Ertan, Rahmiye
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scheme or table
p. 659 - 665
(2010/03/23)
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- Synthesis and antimicrobial activity of some new thiazolyl thiazolidine-2,4-dione derivatives
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In this study, a series of thiazolyl thiazolidine-2,4-dione derivatives (Va-f and VIa-f) were synthesized and evaluated for their antibacterial and antifungal activities against Staphylococcus aureus (ATCC 25923), methicillin resistant S. aureus (MRSA ATC
- Bozdag-Duendar, Oya,Oezgen, Oezen,Mentese, Arzu,Altanlar, Nurten,Atli, Onur,Kendi, Engin,Ertan, Rahmiye
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p. 6012 - 6017
(2008/03/27)
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- The synthesis and characterization of new asymmetrical dihydropyridine derivatives containing a 2,4-dichloro-5-thiazolyl substituent
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Dihydropyridines (DHP) having a heterocyclic aryl substituent at position-4 are calcium channel antagonists. In this report a new group of DHP derivatives with different esters at the C3 and C5 position (asymmetrical diesters) containing 2,4-dichloro-5-thiazolyl at position-4 were synthesized by a condensation reaction of alkyl, cycloalkyl, and aryl acetoacetate in the presence of ammonium acetate in a new shorter pathway. The structure of all compounds was confirmed by IR, 1H NMR, and mass spectrometry. The calcium channel antagonist activity of compounds 6a-6f demonstrated that the compound 6a was the most active compound. Copyright Taylor & Francis Group, LLC.
- Ghodsi, Shahram,Alipour, Eskandar,Amini, Mohsen,Miri, Ramin,Tagi-Ganji, Karim Masoud,Hosseini, Marjan,Mirkhani, Hossein,Shafiee, Abbas
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p. 2435 - 2444
(2007/10/03)
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- Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis
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Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and
- Francisco, Gerardo D.,Li, Zhong,Albright, J. Donald,Eudy, Nancy H.,Katz, Alan H.,Petersen, Peter J.,Labthavikul, Pornpen,Singh, Guy,Yang, Youjun,Rasmussen, Beth A.,Lin, Yang-I.,Mansour, Tarek S.
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p. 235 - 238
(2007/10/03)
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- Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- Azoles. Part 9. Synthesis of Derivatives of Thienothiazole, 4H-Pyrrolothiazole, 2H-Pyrazolothiazole and Isoxazolothiazole from Thiazolidine-2,4-dione
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The aldehyde group of 2,4-dichlorothiazole-5-carbaldehyde was protected and the chlorine atom at position 2 was replaced by hydrogen and a methylthio group, via Cl -> Li exchange, to give 4-chlorothiazole-5-carbaldehyde and its 2-methylthio derivative, re
- Athmani, Salah,Farhat, Mahmoud F.,Iddon, Brian
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p. 973 - 978
(2007/10/02)
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- An Easy General Synthesis of 2-(N,N-Dialkylamino)thiazol-5-yl Aldehydes and Ketones
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Reaction between 2-chloro-5-thiazolyl-lithium and N,N-dialkylformamides or amides gave 2-N,N-dialkylaminothiazol-5-yl aldehydes or ketones on quenching with water.Quenching with acid gave 2-chlorothiazole-5-yl aldehydes or ketones, from which chloride was easily displaced by free amines.
- Sawhney, Indu,Wilson, John R. H.
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p. 329 - 331
(2007/10/02)
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- 2,4-Dichloro-5-thiazolecarboxaldehyde and a process for its preparation
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The new 2,4-dichloro-5-thiazolecarboxaldehyde of the formula STR1 can be prepared in good yields by reacting 2,4-thiazolidinedione (III) with 1-1.5 mol of dimethylformamide and 3-10 mol of phosphorus oxychloride at the reflux temperature of the reaction mixture (about 115° C.) until evolution of HCl gas has ended, and then working up hydrolytically. The aldehyde (II) can readily be converted, via the new oxime (IV), into the corresponding nitrile, 2,4-dichloro-5-cyanothiazole (V), which is a known intermediate for the preparation of herbicidal active compounds of the thiazolyloxyacetamide type.
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