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

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 activit...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1995/10/15, Vol.43(10), pp.1692-1695
Hauptverfasser:	KAMIYA, Shoji, MATSUI, Hiroshi, SHIRAHASE, Hiroaki, NAKAMURA, Shohei, WADA, Katsuo, KANDA, Mamoru, SHIMAJI, Hisanobu, KAKEYA, Nobuharu
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences bronchoconstriction Bronchoconstriction - drug effects Enzyme Inhibitors - pharmacology Guinea Pigs H1-blocker Histamine H1 Antagonists - pharmacology In Vitro Techniques Indoles - pharmacology KY-234 Medical sciences Pharmacology. Drug treatments Platelet Aggregation - drug effects Rabbits Respiratory system structure-activity relationship Thromboxane-A Synthase - antagonists & inhibitors TXA2 synthetase inhibitor
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Zusammenfassung:	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).
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.43.1692