Journal of Medicinal Chemistry p. 1510 - 1515 (1990)
Update date:2022-07-29
Topics:
Atwal
Rovnyak
Schwartz
Moreland
Hedberg
Gougoutas
Malley
Floyd
2-Heterosubstituted-4-aryl-1,4-dihydro-6-methyl-5- pyrimidinecarboxylic acid esters 8, which lack the potential C(s) symmetry of dihydropyridine calcium channel blockers, were prepared and evaluated for biological activity. Biological assays using potassium-depolarized rabbit aorta and radioligand binding techniques showed that some of these compounds are potent mimics of dihydropyridine calcium channel blockers. The combination of a branched ester (e.g. isopropyl, sec-butyl) and an alkylthio group (e.g. SMe) was found to be optimal for biological activity. When compared directly with similarly substituted 2-heteroalkyldihydropyridines 9, dihydropyrimidines 8 were found to be 30-fold less active. The solid-state structure of dihydropyrimidine analogue 8g shows that these compounds can adopt a molecular conformation which is similar to the reported conformation of dihydropyridine calcium channel blockers.
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