A century-old one-pot multicomponent Biginelli reaction products still finds a niche in drug discoveries: Synthesis, mechanistic studies and diverse biological activities of dihydropyrimidines.

• Multicomponent reactions helps to swiftly synthesize and evaluate for activity. • This review covers synthesis of dihydropyrimidines and their biological activities. • Novel dihydropyrimidines can be potential anticancer therapeutics. • This review reports all the patented and marketed dihydropyrimidines as drugs. • This review reports future perspectives of dihydropyrimidines in drug discovery. One of the largest classes of organic molecules are dihydropyrimidines and its derivatives. They are widely used in a variety of pharmacological and industrial applications. Their biological and pharmacological activities include antihypertensive, antidiabetic, anti-inflammatory, antibacterial, antifungal, anticancer, and antiviral activities. The presence of pyrimidine and pyrimidine-containing rings in the substructures of therapeutically effective drugs has drawn considerable interest amongst the scientific fraternity. The potential therapeutic use of these heterocycles has prompted medicinal chemists to synthesize drugs that contain these heterocycles. Against this backdrop, this review examines the one-pot multicomponent reaction, that is, the Biginelli reaction and its mechanism. Also, we reviewed various synthetic approaches for the synthesis of dihydropyrimidines and their diverse pharmacological activities reported in the last two decades. We highlight different marketed drugs with dihydropyrimidine as a pharmacophore as well as patented dihydropyrimidines in the recent past. [Display omitted] [ABSTRACT FROM AUTHOR]