5-HT3 receptor antagonists. 1. New quinoline derivatives

H Hayashi, Y Miwa, I Miki, S Ichikawa…

Index: Hayashi, Hiroaki; Miwa, Yoshikazu; Miki, Ichiro; Ichikawa, Shunji; Yoda, Noboyuki; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 26 p. 4893 - 4902

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Citation Number: 40

Abstract

A series of esters and amides of l-alkyl-2-oxo-l, 2-dihydroquinoline-4-carboxylic acid or 2- alkoxyquinoline-4-carboxylic acid containing a basic azabicycloalkyl moiety has been synthesized and evaluated for affinity for the [3Hlquipazine-labeled 5-HT3 receptors. Most of the esters exhibited 10-fold more potent activity than that of ondansetron (1; Ki= 7.6 nM). Lipophilic substituents at the 1-or 2-position of the quinoline ring enhanced affinity for the ...