Review discusses the synthesis and biological activity of dihydropyrimidinone derivatives, highlighting their potential as antimicrobial agents and drug scaffolds.
Dihydropyrimidinones are heterocycles with a pyrimidine moiety in the ring nucleus, which, in recent decades, have aroused interest in medicinal chemistry due to alleged versatile biological activity. Pyrimidine is one of these heterocyclic compounds having a wide range of biological activity. Pyrimidines are the fundamental structures of nucleic acids, which makes them a better ligand for various biological targets. This review depicts a variety of other pharmacological activities associated with DHPM derivatives, but the main findings are essentially in vitro characteristics of the substances. The spread of incurable diseases, especially infectious diseases caused by antibiotic-resistant bacteria and certain cancers, has become a serious public health concern. Consequently, the search for potent drug scaffolds has played an essential role in drug lead discovery. The multicomponent reaction (MCR) offers a novel method for efficient synthesis. It is rapidly evolving and is important for the discovery of novel molecules. The DHPM biological activities and demonstrates that there is still a need for further in vivo studies to better delineate the pharmacological potential of this class of substances. Articles explore new DHPM derivatives and novel synthetic methods, including green chemistry approaches like the Biginelli reaction. Specific research highlights include the development of DHPM-based bone anabolic agents, antimicrobial compounds targeting drug-resistant bacteria, and their use in developing new materials like dyes and polymers. Biginelli type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. The simplest and most common method for the synthesis of 3, 4-Dihydropyrimidinone was reported first by Biginelli in 1983. It is a one pot three component reaction involving the condensation reaction with Benzaldehyde, Ethylacetoacetate and Urea. This reaction is called as the Biginelli reaction. The conventional Biginelli reaction requires longer reaction time around 18 hrs and also some aldehydes don’t give good yields.
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Kirdat et al. (2025) studied this question.
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