On December 31, 2018, Kaur, Avneet; Pathak, Dharam P.; Sharma, Vidushi; Narasimhan, Balasubramanian; Sharma, Prateek; Mathur, Rajani; Wakode, Sharad published an article.SDS of cas: 99-60-5 The title of the article was Synthesis, biological evaluation and docking study of N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl) benzamide derivatives as selective COX-2 inhibitor and anti-inflammatory agents. And the article contained the following:
A series of N-(2-(3,4,5-trimethoxybenzyl)-benzoxazole-5-yl)benzamide derivatives (3a-3n) was synthesized and evaluated for its in vitro inhibitory activity against COX-1 and COX-2. The compounds with considerable in vitro activity (IC50 < 1 μM), were evaluated in vivo for their anti-inflammatory and ulcerogenic potential. Out of the fourteen newly synthesized compounds; 3b (N-(2-(3,4,5-trimethoxybenzyl)benzoxazol-5-yl)-4-chlorobenzamide), 3d (N-(2-(3,4,5-trimethoxybenzyl)benzoxazol-5-yl)-2-chlorobenzamide), 3e, 3h, 3l and 3m were found to be most potent COX-2 inhibitors in in vitro enzymic assay with IC50 in the range of 0.14-0.69 μM. In vivo anti-inflammatory activity of these six compounds (3b, 3d, 3e, 3h, 3l and 3m) was assessed by carrageenan induced rat paw edema method. The compound 3b (79.54%), 3l (75.00%), 3m (72.72%) and 3d (68.18%) exhibited significant anti-inflammatory activity than standard drug ibuprofen (65.90%). Ulcerogenic activity with histopathol. studies was performed, and the screened compounds demonstrated significant gastric tolerance than ibuprofen. Mol. Docking study was also performed with resolved crystal structure of COX-2 to understand the interacting mechanisms of newly synthesized inhibitors with the active site of COX-2 enzyme and the results were found to be in line with the biol. evaluation studies of the compounds The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).SDS of cas: 99-60-5
The Article related to trimethoxybenzylbenzoxazoleyl benzamide derivative preparation cox2 inhibitor antiinflammatory docking, anti-inflammatory activity, cox-1, cox-2, histopathology, n-(3,4,5-trimethoxybenzyl)benzoxazole, ulcerogenic activity and other aspects.SDS of cas: 99-60-5
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