Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives
| Autor: | Hachio Miyazawa, Atsusuke Terada, Takeshi Oshima, Yoshiya Amemiya, Keiichi Matsuda, Naoko Hatakeyama, Kazuyuki Wachi |
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| Rok vydání: | 1989 |
| Předmět: |
Male
Chemical Phenomena Hydrochloride Stereochemistry Sodium chemistry.chemical_element Thiophenes Inhibitory postsynaptic potential Thromboxane Synthetase Structure-Activity Relationship chemistry.chemical_compound Microsomes Drug Discovery Thromboxane A2 Synthetase Animals Humans Molecular Structure Chemistry Rats Inbred Strains Thiophene derivatives In vitro Rats Molecular Medicine Specific activity Rabbits Thromboxane-A Synthase |
| Zdroj: | Journal of Medicinal Chemistry. 32:1265-1272 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00126a020 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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