Bioorganic and Medicinal Chemistry Letters p. 1797 - 1803 (2018)
Update date:2022-08-05
Topics:
Wei, Zhi-Yu
Chi, Ke-Qiang
Wang, Ke-Si
Wu, Jie
Liu, Li-Ping
Piao, Hu-Ri
Ursolic acid derivatives containing oxadiazole, triazolone, and piperazine moieties were synthesized in an attempt to develop potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, and HRMS. Most of the synthesized compounds showed pronounced anti-inflammatory effects at 100 mg/kg. In particular, compound 11b, which displayed the most potent anti-inflammatory activity of all of the compounds prepared, with 69.76% inhibition after intraperitoneal administration, was more potent than the reference drugs indomethacin and ibuprofen. The cytotoxicity of the compounds was also assessed by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay, and no compounds showed any appreciable cytotoxic activity (IC50 >100 μmol/L). Furthermore, molecular docking studies of the synthesized compounds were performed to rationalize the obtained biological results. Overall, the results indicate that compound 11b could be a therapeutic candidate for the treatment of inflammation.
View MoreNanjing Qirui Material Co., Ltd.
Contact:+86-25-52320053
Address:F4-5, #17 Building, Chuang Yi Yuan, No.6 Guanghua East Street, Nanjing, 210007 P.R.China
Chemtrade International ( China )
Contact:+86-532-86893005
Address:Rm 2-501, Huaxia Zonghe Building, No. 410 JInggangshan Road, Huangdao
HANGZHOU TOYOND BIOTECH CO., LTD
Contact:+86-571-86965177
Address:No. 189, Fengqi East Road, Hangzhou, China
Hongyi Import & Export CO.,LTD
Contact:86-13319649499
Address:Nanzheng Neighborhood Commitees, Chongwen Office, Yongding District
Contact:+86-0592 5353131
Address:No.56 Guani Road Software Park 2,Siming District
Doi:10.1039/b903903a
(2009)Doi:10.1021/ja01119a030
(1953)Doi:10.1007/BF00809689
(1988)Doi:10.1016/j.chemphyslip.2008.12.003
(2009)Doi:10.1021/ja9032132
(2009)Doi:10.1021/ja01196a011
(1947)