Preliminary finding on a new calcium channel entry blocker chemotype: 5,6-diamino-4-hydroxy-2-mercaptopyrimidine derivatives.

ABSTRACT

We report the preliminary in vitro characterization of a series of pyrimidines as a new chemotype that modulates cardiovascular parameters and relaxes ileum smooth muscle according to classical calcium entry blockers. Tested compounds showed an interesting negative inotropic selectivity. In patch-clamp experiments they block L- over T-type calcium currents. Two requisites seem essential for the activity lipophilic substituents in positions 2 and 5 of the pyrimidine ring and the acetamidic function in position 6.