Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.

Article Details

Citation

Amemiya Y, Terada A, Wachi K, Miyazawa H, Hatakeyama N, Matsuda K, Oshima T

Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.

J Med Chem. 1989 Jun;32(6):1265-72.

PubMed ID
2724299 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DazoxibenThromboxane-A synthaseIC 50 (nM)620N/AN/ADetails
DazoxibenThromboxane-A synthaseIC 50 (nM)106N/AN/ADetails