On February 15, 2018, Kaur, Avneet; Pathak, Dharam P.; Sharma, Vidushi; Wakode, Sharad published an article.Related Products of 99-60-5 The title of the article was Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents. And the article contained the following:
A new series of substituted-N-(3,4-dimethoxyphenyl)-benzoxazole derivatives 13a-13p was synthesized and evaluated in vitro for their COX (I and II) inhibitory activity, in vivo anti-inflammatory and ulcerogenic potential. Compounds 13d, 13h, 13k, 13l and 13n exhibited significant COX-2 inhibitory activity and selectivity towards COX-2 over COX-1. These selected compounds were screened for their in vivo anti-inflammatory activity by carrageenan induced rat paw edema method. Among these compounds, 13d (2-chloro-N-(2-(3,4-dimethoxyphenyl)benzoxazol-5-yl)benzamide) was the most promising analogs of the series with percent inhibition of 84.09 and IC50 value of 0.04 μM and 1.02 μM (COX-2 and COX-1) resp. Furthermore, ulcerogenic study was performed and tested compounds (13d, 13h, 13k, 13l) demonstrated a significant gastric tolerance than ibuprofen. Mol. docking study was also performed with resolved crystal structure of COX-2 to understand the binding mechanisms of newly synthesized inhibitors in the active site of COX-2 enzyme and the results were found to be concordant with the biol. evaluation studies of the compounds These newly synthesized inhibitors also showed acceptable pharmacokinetic profile in the in silico ADME/T analyses. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Related Products of 99-60-5
The Article related to benzoxazole derivative preparation cyclooxygenase cox2 inhibitor antiinflammatory ulcer, anti-inflammatory activity, benzoxazole derivatives, selective cox-2 inhibitors, ulcerogenic liability and other aspects.Related Products of 99-60-5
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Chlorides – an overview | ScienceDirect Topics