140890-68-2Relevant academic research and scientific papers
New prenylamine-analogues: investigations of their influence on calcium-dependent biological systems
Caldirola, P.,Zandberg, P.,Mannhold, R.,Timmerman, H.
, p. 555 - 568 (1993)
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
Benzhydryl derivatives having calmodulin inhibitor properties
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, (2008/06/13)
The invention relates to a benzhydryl derivative having the formula STR1 wherein each of the groups R1, R2, and R3 represents one to four substituents independently selected from the group consisting of hydrogen, lower alkyl, halogen, and CF3, and at least one of the groups R1, R2, and R3 is halogen or CF3 ; R4 represents hydrogen or methyl; n is 2, 3, or 4; m is 1, 2, or 3; and X represents O or S; or its pharmaceutically acceptable salts. The benzhydryl derivative of the invention can be used to treat patients who are suffering from diseases which are influenced by calmodulin.
