Bioorganic Chemistry p. 191 - 202 (2018)
Update date:2022-08-03
Topics:
Kaur, Avneet
Pathak, Dharam P.
Sharma, Vidushi
Narasimhan, Balasubramanian
Sharma, Prateek
Mathur, Rajani
Wakode, Sharad
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, 3d, 3e, 3h, 3l and 3m were found to be most potent COX-2 inhibitors in in vitro enzymatic 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 histopathological studies was performed, and the screened compounds demonstrated significant gastric tolerance than ibuprofen. Molecular 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 biological evaluation studies of the compounds.
View MoreContact:18669908765
Address:Zibo City, Shandong Province, P.R.China
PharmaResources(Kaiyuan)CO,.Ltd
Contact:+86-21-50720028
Address:No.3, Beihuan Road, Economic Development District, Kaiyuan City, Tieling City, Liaoning Province, China 112300
Ningbo Inno Pharmchem Co., Ltd.
Contact:86-574-87319282
Address:6F-5,NO.163 RUIQING RD.,NINGBO 315000 CHINA
Nanjing Xi Ze Biological Technology Co., Ltd
Contact:86-025-66023220
Address:Address: Nanjin Qixia District Maigaoqiao R & D base in Pioneer Park Chun Yin Road 18-A928
Shandong Shouguang Songchuan Industrial Additives Co.,Ltd
Contact:+86-536-8566856
Address:Shouguang,Shandong,China
Doi:10.1080/00397919508011770
(1995)Doi:10.1080/15257779508014659
(1995)Doi:10.1016/j.chembiol.2019.03.008
(2019)Doi:10.1016/S0040-4039(00)76871-7
(1994)Doi:10.14233/ajchem.2014.16438
(2014)Doi:10.1002/chem.202000859
(2020)