Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review

Abstract

Dihydropyrimidines are the most important heterocyclic ring systems which play an important role in the synthesis of DNA and RNA. Synthetically they were synthesized using Multi-component reactions like Biginelli reaction and Hantzschdihydropyridine. 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 anti-inflammatory, anti-HIV, anti-tubercular, antifungal anticancer, antibacterial, antifilarial, antihyperglycemic, antihypertensive, analgesic, anti-convulsant, antioxidant, anti-TRPA1, anti-SARS, and anti-cancer activity and α binding affinity.

Enantioselective Brønsted Acid Catalysis as a Tool for the Synthesis of Natural Products and Pharmaceuticals

“…Biginelli reaction [45] 3,4-Dihydropyrimidin-2-(1H)-ones (DHPMs)a re heterocylic moieties encountered in the structure of numerous bioactive molecules. [46] Since its discovery at the end of the 19th century, Scheme14. Synthesis of pyrroloquinolones.…”

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications

“…The N-heterocyclic skeletons feature significantly various classes of therapeutic applications and are used as the building blocks of a number of new drug candidates, due to the ability of the nitrogen atom to easily form hydrogen bonding with biological targets [15][16][17]. For example, pyrimidine derivatives have various therapeutic applications in medicinal chemistry and pyrimidine skeleton of thymine, cytosine, and uracil are essential building blocks of nucleic acids, DNA and RNA [18]. A vast number of nitrogen-containing heterocyclic compounds are known to exhibit a wide range of pharmacological activities including anticancer, anti-HIV, antimalaria, anti-tubercular, anti-microbial and diabetic activities [19][20][21][22][23][24][25].…”

Ethyl 4-(2-fluorophenyl)-6-methyl-2-thioxo-1-(p-tolyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate

“…The Biginelli reaction involves the acid-catalyzed multicomponent synthesis of 3,4dihydropyrimidin-2(1H)-ones(thiones) (DHPMs) [1]. Thus, this reaction is a powerful tool for the fast and easy generation of libraries with great structural diversity [2].…”