Inhibitors of cyclic AMP phosphodiesterase. 1. Analogs of cilostamide and anagrelide

GH Jones, MC Venuti, R Alvarez, JJ Bruno…

Index: Jones; Venuti; Alvarez; Bruno; Berks; Prince Journal of Medicinal Chemistry, 1987 , vol. 30, # 2 p. 295 - 303

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Citation Number: 46

Abstract

Evaluation of a series of lactam heterocyclic analogues of cilostamide (2) as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their corresponding methoxy-substituted heterocycles has revealed that the N-cyclohexyl-N-methyl-4-oxybutyramide side chain of 2 is an important lipophilic and/or steric pharmacophore. Attachment of this side chain to the parent heterocycle of the potent ...