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Abstract
In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) via
three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate
was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type
dihydropyrimidones have received a considerable amount of attention due to the interesting
pharmacological properties associated with this heterocyclic scaffold. In this review,
we highlight recent developments in this area, with a focus on the DHPMs recently
developed as calcium channel modulators, alpha(1a) adrenoceptor-selective antagonists
and compounds that target the mitotic machinery.