Synthesis, biological evaluation, docking study and ulcerogenicity profiling of some novel quinoline-2-carboxamides as dual COXs/LOX inhibitors endowed with anti-inflammatory activity

详细信息    查看全文

• 作者：Mostafa H. Abdelrahman^a ; Bahaa G.M. Youssif^b ; ^c ; ^{bgyoussif@ju.edu.sa} ; Mohamed A. abdelgawad^c ; ^d ; Ahmed H. Abdelazeem^e ; ^f ; Hussein M. Ibrahim^g ; ^h ; Abd El Ghany A. Moustafa^h ; ⁱ ; Laurent Treamblu^j ; Syed Nasir Abbas Bukhari^c ; ^{snab_hussaini@yahoo.com}
• 关键词：Quinoline-2-carboxamides ; COXs ; LOX ; Docking ; Anti-inflammatory
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：972-985
• 全文大小：4290 K
• 卷排序：127

文摘

A new series of novelquinoline-2-carboxamides was synthesized. New compounds were evaluated in vitro as dual COXs/LOX inhibitors. Compounds 19 and 27 exhibited the highest potency and selectivity for COX-2 inhibitory activity. Two compounds (19 and 27) have a superior gastric safety profile comparable to indomethacin.