title: Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
abstract: 1-Imidazolylalkyl-substituted di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives and related compounds were synthesized from tetrahydrobenzo[b]thiophene derivatives (1 or 4) in order to study the structure-activity relationships of the inhibition of thromboxane A2 synthetase in vitro. Sodium 2-(1-imidazolylmethyl)-4,5-dihydrobenzo[b]thiophene-6-carboxylate (26) and 2-(1-imidazolylmethyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-6-carbo xylic acid hydrochloride (28) showed the most potent and specific activity in vitro for thromboxane A2 synthetase inhibition.
authors.affiliation: Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Amemiya
authors.forename: A
authors.initials: A
authors.lastname: Terada
authors.forename: K
authors.initials: K
authors.lastname: Wachi
authors.forename: H
authors.initials: H
authors.lastname: Miyazawa
authors.forename: N
authors.initials: N
authors.lastname: Hatakeyama
authors.forename: K
authors.initials: K
authors.lastname: Matsuda
authors.forename: T
authors.initials: T
authors.lastname: Oshima
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D008297:Male; D008861:Microsomes / Q000201:enzymology; D015394:Molecular Structure; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*
chemical_list: D013876:Thiophenes; D013930:Thromboxane-A Synthase