Harada, Hiroshi published the artcileDevelopment of potent serotonin-3 (5-HT3) receptor antagonists. I. Structure-activity relationships of 2-alkoxy-4-amino-5-chlorobenzamide derivatives, Related Products of chlorides-buliding-blocks, the publication is Chemical & Pharmaceutical Bulletin (1995), 43(8), 1364-78, database is CAplus and MEDLINE.
A new series of 2-alkoxy-4-amino-5-chlorobenzamide derivatives bearing 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 von Bezold-Jarisch reflex in rats. The five- to seven-membered heterocycles 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-ethoxybenzamide and the 1-benzyl-4-methylhexahydro-1H-1,4-diazepine analog showed potent 5-HT3 receptor antagonist activity without 5-HT4 receptor binding affinity.
Chemical & Pharmaceutical Bulletin published new progress about 36335-47-4. 36335-47-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Ether, name is 3-Chloro-2,6-dimethoxybenzoic acid, and the molecular formula is C9H9ClO4, Related Products of chlorides-buliding-blocks.
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