Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide- …

…, H Oda, S Harada, Y Sugimoto, K Sasaki…

Index: Kakuta, Hiroki; Zheng, Xiaoxia; Oda, Hiroyuki; Harada, Shun; Sugimoto, Yukio; Sasaki, Kenji; Tai, Akihiro Journal of Medicinal Chemistry, 2008 , vol. 51, # 8 p. 2400 - 2411

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Citation Number: 60

Abstract

Although cyclooxygenase-1 (COX-1) inhibition is thought to be a major mechanism of gastric damage by nonsteroidal anti-inflammatory drugs (NSAIDs), some COX-1-selective inhibitors exhibit strong analgesic effects without causing gastric damage. However, it is not clear whether their analgesic effects are attributable to COX-1-inhibitory activity or other bioactivities. Here, we report that N-(5-amino-2-pyridinyl)-4-(trifluoromethyl) benzamide ( ...