Design and synthesis of 6-chloro-3, 4-dihydro-4-methyl-2H-1, 4-benzoxazine-8-carboxamide derivatives as potent serotonin-3 (5-HT3) receptor antagonists.

T KUROITA, M SAKAMORI, T KAWAKITA

Index: Kuroita, Takanobu; Sakamori, Masamitsu; Kawakita, Takeshi Chemical and Pharmaceutical Bulletin, 1996 , vol. 44, # 4 p. 756 - 764

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Citation Number: 38

Abstract

Several 3-substituted 5-chloro-2-methoxybenzamides were synthesized and evaluated for serotonin-3 (5-HT-3) receptor binding affinity. The 5-HT 3 receptor antagonistic activity of zacopride, a representative 5-HT 3 receptor antagonist, was unchanged by the replacement of the 4-amino substituent on the aromaitc moiety by a 3-dimethyl-amino substituent. This finding prompted a structural modification of azasetron, another 5-HT 3 receptor ...