39884-16-7Relevant academic research and scientific papers
Chalcone-Thiazole Hybrids: Rational Design, Synthesis, and Lead Identification against 5-Lipoxygenase
Doble, Mukesh,Manju, S. L.,Sinha, Shweta
, (2019)
A hybrid pharmacophore approach is used to design and synthesize novel chalcone-thiazole hybrid molecules. Herein, thiazole has been hybridized with chalcone to obtain a new class of 5-LOX inhibitors. In vitro biological evaluation showed that most of the compounds were better 5-LOX inhibitors than the positive control, Zileuton (IC50 = 1.05 ± 0.03 μM). The best compounds in the series, namely, 4k, 4n, and 4v (4k: IC50 = 0.07 ± 0.02 μM, 4n: IC50 = 0.08 ± 0.05 μM, 4v: 0.12 ± 0.04 μM) are found to be 10 times more active than previously reported 2-amino thiazole (2m: IC50 = 0.9 ± 0.1 μM) by us. Further, 4k has redox (noncompetitive) while 4n and 4v act through a competitive inhibition mechanism. SAR indicated that the presence of methoxy/methyl either in the vicinity of chalcone or both thiazole and chalcone contributed to the synergistic inhibitory effect.
N-(5-acetyl-4-methylthiazol-2-yl)arylamide derivatives as multi-target-directed ligands: design, synthesis, biochemical evaluation and computational analysis
Channar, Kashif Ali,Channar, Pervaiz Ali,Ejaz, Syeda Abida,Indher, Hafiz Abdul Bari,Ismail, Hammad,Mahmood, Hafiz Mohammad Kashif,Rafiq, Mamoona,Saeed, Aamer,Saeed, Amna,Saeed, Shomaila,Ujan, Rabail
, (2022/01/19)
In the present study, we are reporting the synthesis of a total eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives (3a-h). The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship. All the synthesized compounds were further subjected to chemical characterization (NMR, FTIR and elemental analysis) and further tested for biological activities (antioxidant, antibacterial, antifungal and α-glucosidase). The anti-oxidant properties of compound 3h (IC50 ± SEM = 141.9 ± 1.12?μg/mL) were found maximum in comparison to the rest of the derivatives. The antibacterial results showed the compounds 3d and 3h as a significant bacterial inhibitor. The significant fungicidal activity was observed by compound 3a with the zone of inhibition up to 24 mm which in comparison with the results of positive control (Terbinafine). When the effect was observed on α-glucosidase activity, the highest enzyme inhibition activity was observed by 3h (IC50 ± SEM 134.4 ± 1.01?μg/mL) followed by 3c (IC50 ± SEM = 157.3 ± 1.11?μg/mL). The results were further supported by molecular docking studies and the chemical stability of the derivatives was also performed by density functional theory (DFTs) calculations. The data revealed that most of the derivatives are multi-target ligands and can be used as lead molecules for the synthesis of derivatives for their further evaluation at molecular targets for the treatment of specific diseases. Graphical abstract: [Figure not available: see fulltext.] Synopsis This article reports the synthesis of a total of eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives. The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship.
Synthesis, Characterization, Crystal Structure and Biological Study of Carboxamides Obtained from 2-Aminothiazole Derivatives
Wazalwar, Sachin S.,Banpurkar, Anita R.,Perdih, Franc
, p. 319 - 329 (2019/07/29)
Abstract: Two series of novel thiazolylcarboxamide derivatives were synthesized by the reaction of ethyl 2-amino-4-methylthiazole-5-carboxylate or 1-(2-amino-4-methylthiazol-5-yl)ethan-1-one with four substituted carbonyl chlorides at 0?°C in excellent yi
5-(3-phenylacryloyl)-2-benzoylaminothiazole and medical use thereof
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Paragraph 0042; 0043; 0055; 0057; 0058; 0059, (2018/12/02)
The invention relates to 5-(3-phenylacryloyl)-2-benzoylaminothiazole represented by formula I, pharmaceutically acceptable salts and a medicinal composition thereof, an application thereof in the preparation of influenza virus neuraminidase inhibitors. In
