Collect. Czech. Chem. Commun. 1992, 57, 1967-1981

Some New Analogues of Verapamil and Mepamil. Synthesis and Basic Pharmacological Properties

Gabriel Butora, Ludvík Bláha, Miroslav Rajšner and Ivan Helfert

Research Institute for Pharmacy and Biochemistry, 130 60 Prague


Some new analogues of verapamil (Ia) and mepamil (Ib), calcium antagonists of arylalkylamine type, were synthesized and screened for cardiovascular activities. The basic structure was modified a) on the phenyl ring, attached to the quaternary carbon, b) on the alkyl group, attached to the quaternary carbon and c) on the alkylamino group, attached in position 3 to the n-propyl fragment. Except of 2-(2-chlorophenyl)-2-isopropyl-5-(N-methylhomoveratrylamino)valeronitrile (VIa), all the synthesized compounds exhibited lower hypotensive activity, than the mother compound, verapamil.