I. Adachi, T. Yamamori, Y. Hiramatsu
Nov 25, 1988
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0
Influential Citations
49
Citations
Quality indicators
Journal
Chemical & pharmaceutical bulletin
Abstract
A series of 4-aryl-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate derivatives(I)was synthesized and tested for binding affinity to Ca2 channels in rat cerebral cortex membranes, coronary vasodilator effect in isolated guinea pig hearts,and antihypertensive activity in spontaneously hypertensive rats.Several compounds had potent coronary vasodilator and antihypertensive activities.The structure-ctivity relationships of the series indicated that a lipophilic 3alkyl substituent with moderate bulkiness was effective for enhancing the pharmacological potencies.Among them, methyl 4,7-dihydro-3-isobuty1-6-methy1-4-(3-nitrophenyl)thieno[2,3-Mpyridine-5-carboxylate(S-312)was selected as a promising cardiovascular agent.The relationship between the absolute configuration of S-312 and its biological activities is also presented.