Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Studies on Dihydropyridines. III. Synthesis of 4, 7-Dihydrothieno [2, 3-b]-pyridines with Vasodilator and Antihypertensive Activities
IKUO ADACHI, TERUO YAMAMORI, YOSHIHARU HIRAMATSU, KATSUNORI SAKAI, SHIN-ICHI MIHARA, MASARU KAWAKAMI, MASAO MASUI, OSAMU UNO, MOTOHIKO UEDA
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Keywords: thieno [2, 3-b] pyridine, calcium antagonist, vasodilator activity, antihypertensive activity
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1988 Volume 36 Issue 11 Pages 4389-4402

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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 3-alkyl 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-b] pyridine-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.

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