Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
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.
Amemiya
Y
Y
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Terada
A
A
Wachi
K
K
Miyazawa
H
H
Hatakeyama
N
N
Matsuda
K
K
Oshima
T
T
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*
D013876:Thiophenes; D013930:Thromboxane-A Synthase