Thromboxane A2 Synthetase Inhibitors with Histamine H1-Blocking Activity : Synthesis and Evaluation of a New Series of Indole Derivatives

Shoji KAMIYA; Hiroshi MATSUI; Hiroaki SHIRAHASE; Shohei NAKAMURA; Katsuo WADA; Mamoru KANDA; Hisanobu SHIMAJI; Nobuharu KAKEYA

doi:10.1248/cpb.43.1692

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

著者情報

キーワード: TXA₂ synthetase inhibitor, H₁-blocker, bronchoconstriction, structure-activity relationship, KY-234

ジャーナルフリー

1995 年 43 巻 10 号 p. 1692-1695

DOI https://doi.org/10.1248/cpb.43.1692

詳細

抄録

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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