An efficacious protocol for C-4 substituted 3,4-dihydropyrimidinones. Synthesis and calcium channel binding studies.

ABSTRACT: Ethyl 1,2-dihydro-1,6-dimethyl/6-methyl-2-oxopyrimidine-5-carboxylates react with C-nucleophiles as well as anion of enantiopure chiral auxiliary (1R,2S,5R)-(-)-methyl (S)-p-toluenesulfinate to afford C-4 substituted and enantiopure congeners of medicinally potent Biginelli dihydropyrimidinones. The calcium channel blocking activity of some of the compounds was evaluated and compared with nifedipine for their ability to relax a membrane depolarization induced contraction.

SUBMITTER: Singh K 

PROVIDER: S-EPMC3834990 | biostudies-literature | 2009 Jul

REPOSITORIES: biostudies-literature