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Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-1,2,4-triazol-1-yl)alkyl]aryl amides.

Abstract：

:The title compounds were prepared to investigate their potential as thromboxane synthetase inhibitors as well as antihypertensive agents. Imidazoles VIII and triazoles X were prepared to examine the effects of aromatic substitution, chain length, and heterocycle substitution upon biological activity. Imidazoles VIII and triazoles X were thromboxane synthetase inhibitors that did not inhibit prostacyclin formation. The most interesting thromboxane synthetase inhibitors prepared were 4-chloro-, 4-(trifluoromethyl)-, and 4-bromobenzamide derivatives of (1H-imidazol-1-yl)alkylamines with C5-C8 alkyl chains separating the heterocycle from the amide moiety, while the most active antihypertensive agents were 3- or 4-chloro-, -bromo, or -(trifluoromethyl)benzamides with C3 alkyl chains. The best thromboxane synthetase inhibitors in this study were up to 10 times more potent than the standard, dazoxiben (UK 37,248).

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Wright WB Jr,Press JB,Chan PS,Marsico JW,Haug MF,Lucas J,Tauber J,Tomcufcik AS

doi

10.1021/jm00154a017

subject

Has Abstract

pub_date

1986-04-01 00:00:00

pages

523-30

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

29

pub_type

杂志文章

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