Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Thromboxane A2 Synthetase Inhibitors with Histamine H1-Blocking Activity : Synthesis and Evaluation of a New Series of Indole Derivatives
神谷 尚治松井 博白波瀬 弘明中村 正平和田 勝夫神田 守嶋路 久延掛谷 宣治
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1995 年 43 巻 10 号 p. 1692-1695

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A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A2 (TXA2) synthetase-inhibitory and histaminergic H1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positioal isomers of carboxylic acid. 1-[3-(4-Benzhyrdyl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6-carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC50=5×10-8M) and H1-blocking activity (IC50=8×10-9M).
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© The Pharmaceutical Society of Japan
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