Studies on Dihydropyridines. II. : Synthesis of 4,7-Dihydropyrazolo[3,4-b]-pyridines with Vasodilating and Antihypertensive Activities(Medeicinal Chemistry,Chemical)

概要

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A series of 4-aryl-4,7-dihydropyrazolo[3,4-b]pyridine-5-carboxylate derivatives (72-149) was prepared and the compounds were tested for Ca-blocking activity in isolated guinea pig portal vein, antihypertensive activity in spontaneously hypertensive rats, and coronary vasodilaling effect in isolated guinea pig heart. A number of derivatives had potent antihypertensive and coronary vasodilating activities. The structure-activity relationships of the series indicated that a 3-cyclopentyl or 3-cyclohcxyl substituent and a hydrophobic 5-ester moiety with moderate bulkiness were effective for increasing the pharmacological potencies.
公益社団法人日本薬学会の論文
1987-08-25