Biologically active dihydropyrimidones of the Biginelli-type — a literature survey

In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1 H)-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, α 1a adrenoceptor-selective antagonists and compounds that target the mitotic machinery.