کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1359392 | 981401 | 2014 | 6 صفحه PDF | دانلود رایگان |
A series of 1,3,4-trisubstituted pyrazole derivatives (3a–f), (4a–f), and (5a–f) have been synthesized and evaluated for their cyclooxygenase (COX-1 and COX-2) inhibitory activity. The structures of newly synthesized compounds were characterized by IR, 1H NMR, and mass spectral analysis. All of the compounds showed good inhibition of COX-2 with IC50 of 1.33–17.5 μM. Among these derivatives, compound (5c) was the most potent and selective COX-2 inhibitor (IC50 = 1.33 μM), with a significant selectivity index (SI >60). Molecular docking studies were carried out in order to predict the hypothetical binding mode of these compounds to the COX-2 isoenzyme. The result of present study suggests that pyrazole–thiadiazole hybrid could be an interesting approach for the design of new selective COX-2 inhibitory agents.
A novel class of pyrazole derivatives have been synthesized and investigated for their in vitro cyclooxygenase inhibitory and cytotoxicity activities. Compound 5c showed potential selective COX-2 inhibitory activity.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 22, 15 November 2014, Pages 5324–5329