Long-acting dihydropyridine calcium antagonists. 9. Structure activity relationships around amlodipine

…, JE Arrowsmith, SF Campbell, PE Cross

Index: Alker, D; Arrowsmith, JE; Campbell, SF; Cross, PE European Journal of Medicinal Chemistry, 1991 , vol. 26, # 9 p. 907 - 913

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Citation Number: 17

Abstract

Abstract The preparation of a range of 1, 4-dihydropyridine analogues of amlodipine has been undertaken and their calcium antagonist activities on rat aorta have been evaluated. Increasing the size of the C5 ester group dramatically reduces calcium antagonist activity, a trend which would be compatible with the carbonyl group of that ester binding to the DHP receptor. Amlodipine analogues with extended C3 ester substituents also have lower ...