Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-inflammatory agents.
To improve the medicinal activity, the structure of diflunisal has been modified. Twenty-one amide derivatives of diflunisal were synthesized starting from diflunisal in three steps with total yields from 72% to 89%. All compounds were identified by (1)H NMR, MS, and elemental analysis. The anti-inflammatory and analgesic activities for 19 compounds were evaluated. It was found that 5m possesses an excellent anti-inflammatory activity and a good analgesic activity, maybe a potential anti-inflammatory agent.
Zhong
Guang-Xiang
GX
College of Pharmaceutical Science, Zhejiang University of Technology, 18, Chaowang Road, Hangzhou, Zhejiang 310032, China. drzhonggx@sohu.com
Hu
Jin-Qing
JQ
Zhao
Kun
K
Chen
Lu-Lu
LL
Hu
Wei-Xiao
WX
Qiu
Ming-You
MY
D000577:Amides / Q000737:chemistry*; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004061:Diflunisal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry
D000577:Amides; D000893:Anti-Inflammatory Agents; D004061:Diflunisal