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(Received December 19, 1986) 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 vasodilating 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 3cyclopentyl or 3-cyclohexyl substituent and a hydrophobic 5-ester moiety with moderate bulkiness were effective for increasing the pharmacological potencies.

Studies on dihydropyridines. II. Synthesis of 4,7-dihydropyrazolo(3,4-b)pyridines with vasodilating and antihypertensive activities.