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[Quinazolinones. 16. Synthesis and in vitro pharmacology of 2-aryl-1- ([3-(imidazol-4-yl)propyl]-guanidinylalkyl)-2,3-dihydro-4(1H)- quinazolinones].

作者信息

Büyüktimkin S, Buschauer A, Schunack W

出版信息

Arch Pharm (Weinheim). 1989 Feb;322(2):115-8. doi: 10.1002/ardp.19893220212.

Abstract

A series of 2-aryl-1- ([3-(imidazol-4-yl)propyl]guanidinylalkyl)-2,3-dihydro-4(1H)- quinazolinones were prepared starting with appropriate aminoalkyl-quinazolinones. The substances proved to be moderate H1-antagonists at the isolated guinea-pig ileum as well as H2-agonists, maximally achieving 1.6 times the activity of histamine at the isolated guinea-pig right atrium. Compounds with a three-membered carbon chain connecting the bicyclus and the guanidine system are up to 100 times more active at the atrium (chronotropic effect) than the corresponding lower homologues.

摘要

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