Pyrimidine-based antimalarials: design strategies and antiplasmodial effects

Abstract

The versatility in the design strategies of pyrimidine scaffold offer considerable opportunity for developing antimalarials capable of hitting different biological targets.

HClO4‐Al2O3 as a Prominent Catalyst in the Synthesis of 3,4‐Dihydropyrimidin‐2(1H)‐ones/thiones under Environmentally Friendly Solvent Conditions

“…[5] Another relevant aspect is the biological properties presented by DHPMs/thiones. There are reports in the literature of several biological activities, including antibacterial, [6] antifungal, [7] antitubercular, [8] anti-inflammatory, [9] antioxidant, [10] inhibition of acetylcholinesterase acting on Alzheimer's disease, [11] antitumoral, [12] antimalarial, [13] against HIV-1, [14] among others.…”

Design of antimalarial agents based on pyrimidine derivatives as methionine aminopeptidase 1b inhibitor: Molecular docking, quantitative structure activity relationships, and molecular dynamics simulation studies

“…Docking protocols help elucidate the most energetically calculated favorable binding pose of a ligand to the receptor . Pyrimidine nuclei are used as antimalarial agents; this pharmacophore was used in hybrids with other compounds such as 4‐aminoquinoline‐pyrimidine hybrids, N ‐substituted 4‐aminoquinoline‐pyrimidine hybrids, primaquine pyrimidine hybrids, quinoline–pyrimidine hybrids, and isoxazole pyrimidine and was evaluated as an antimalarial agent …”

Ag2O on ZrO2 as a Recyclable Catalyst for Multicomponent Synthesis of Indenopyrimidine Derivatives

“…In the N-heterocyclic class of scaffolds, pyrimidine and its derivatives play a prominent role [ 11 ]. Being the main constituents of several natural products, these pyrimidines represent a significant class of molecules which have been of increased interest in recent years owing to their valuable pharmacological and biological applications in antimicrobial [ 12 ], antifungal [ 13 ], anti-tumor [ 14 ], anti-HIV [ 15 ], anti-tubercular [ 16 ], anti-inflammatory [ 17 ], and antimalarial [ 18 ] activities. Moreover, aryl-indenopyrimidines have been used as adenosine A2A receptor antagonists [ 19 ], which are useful, and many reports have dealt with the preparation of different types of pyrimidine derivatives via multicomponent reactions.…”