Studies on dihydropyridines. III. Synthesis of 4,7-dihydrothieno [2,3-b]-pyridines with vasodilator and antihypertensive activities.

doi:10.1248/CPB.36.4389

Paper

Studies on dihydropyridines. III. Synthesis of 4,7-dihydrothieno [2,3-b]-pyridines with vasodilator and antihypertensive activities.

Published Nov 25, 1988 · I. Adachi, T. Yamamori, Y. Hiramatsu

Chemical & pharmaceutical bulletin

51

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0

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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.

Non-RCTAnimal Study

Study Snapshot

The synthesized 4,7-dihydrothieno[2,3-b]-pyridine derivatives show potent coronary vasodilator and antihypertensive activities, with methyl 4,7-dihydro-3-isobuty1-6-methy1-4-(3

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Studies on dihydropyridines. III. Synthesis of 4,7-dihydrothieno [2,3-b]-pyridines with vasodilator and antihypertensive activities.

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