Chemical and Pharmaceutical Bulletin p. 1364 - 1378 (1995)
Update date:2022-07-31
Topics:
Harada
Morie
Hirokawa
Yoshida
Kato
A new series of 2-alkoxy-4-amino-5-chlorobenzamide derivatives hearing five- to seven-membered heteroalicyclic rings in the amine moiety was synthesized and evaluated for serotonin-3 (5-HT3) receptor antagonistic activity by assaying the ability to antagonize the yon Bezold-Jarisch reflex in rats. The five- to seven-membered heteroalicycles comprise pyrrolidine, morpholine, 1,4-thiazine, piperidine, piperazine, 1,4-oxazepine, 1,4- thiazepine, azepine, and 1,4-diazepine rings. Among them, some benzamide derivatives having a 1,4-diazepine ring showed a potent 5-HT3 receptor antagonistic activity. In particular, 4-amino-5-chloro-N-(1,4- dimethylhexahydro-1H-1,4-diazepin-6-yl)-2-ethoxyhenzamide (96) and the 1- benzyl-4-methylhexahydro-1H-1,4-diazepine analogue 103 showed potent 5-HT3 receptor antagonistic activity without 5-HT4 receptor binding affinity.
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