5-HT3 Receptor antagonists. 2. 4-Hydroxy-4-quinolinecarboxylic acid derivatives

…, Y Miwa, S Ichikawa, N Yoda, I Miki, A Ishii…

文献索引：Hayashi; Miwa; Ichikawa; Yoda; Miki; Ishii; Kono; Yasuzawa; Suzuki Journal of medicinal chemistry, 1993 , vol. 36, # 5 p. 617 - 626

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被引用次数: 40

摘要

Chydroxy-2-oxo-l, 2-dihydro-3-quinolinecarboxamide derivatives (7a) exhibited higher affinity (eg, 7d Ki= 0.48 nM) for the 5-HT3 receptors than ondaneetron (Ki= 7.6 nM) or granisetron (Ki= 2.1 nM), these amides showed less potent activity in the BJ reflex test than the reference compounds. Interestingly, the ester derivatives 7c, 7f, and 7h eliminated affinity for the 5-HT3 receptors. These unusual structure-activity relationships and the deviation of ...