New prenylamine-analogues: investigations of their influence on calcium-dependent biological systems

Article abstract of DOI:10.1016/0223-5234(93)90086-T

Chemically, prenylamine belongs to the diphenylalkylamine class.Compounds of this class are calcium antagonists with broad spectrum of activities due to their influence on both extracellular and intracellular sites.In the present study the calcium antagonistic profile of a recently developed new series of prenylamine analogues has been investigated using different in vitro systems.The inhibiting concentrations for the most active compound are ca. 1.5 μM; several derivatives are inactive up to a concentration of 10 μM.Structural modifications towards an increase oflipophilicity make these molecules interact (inhibition) with the intracellular calcium-binding protein calmodulin; for the series no correlation between calcium-blocking and calmodulin antagonistic effects has been found. - Keywords: prenylamine derivatives /diphenylalkylamines /calcium antagonists / calmodulin antagonists / qualitative structure-activity relationship