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In the armamentarium of calcium channel blockers appropriately functionalized 3,4-dihydropyrimidin-2(1H)- ones have received considerable attention in recent past owing to their structural similarity with 1,4-dihydropyridine based drugs. In this review, we highlight detailed investigations in the calcium channel blocking and other activities of this category of compounds as well as trace their genesis from 1,4-dihydropyridine based drugs.