Synthesis and Pharmacological Activities of Chalcone and Its Derivatives Bearing N-Heterocyclic Scaffolds: A Review

Abstract

The incorporation of heterocyclic moieties into the standard chemical structure with a biologically active scaffold has become of crucial practice for the construction of pharmacologically potent candidates in the drug arena. Currently, numerous kinds of chalcones and their derivatives have been synthesized using the incorporation of heterocyclic scaffolds, especially chalcones bearing heterocyclic moieties that display improved efficiency and potential for drug production in pharmaceutical sectors. The current Review focuses on recent advances in the synthetic approaches and pharmacological activities such as antibacterial, antifungal, antitubercular, antioxidant, antimalarial, anticancer, antiinflammatory, antigiardial, and antifilarial activities of chalcone derivatives incorporating N-heterocyclic moieties at either the A-ring or B-ring.

Crystal structure and Hirshfeld surface analysis of (2E)-1-phenyl-3-(1H-pyrrol-2-yl)propen-1-one

“…(Walsh et al, 2006;Sobhi & Faisal, 2023). Chalcones incorporating N-heterocyclic, especially pyrrole, scaffolds with various biological and pharmacological activities, such as antioxidant, antibacterial, antifungal, antileishmanial, anticancer, antitubercular, antimalarial and other properties, have been reviewed recently (Mezgebe et al, 2023). In addition, the incorporation of diverse pharmacophore groups in a pyrrole scaffold has led to the development of more desired compounds, such as elopiprazole, lorpiprazole, isamoltane, obatoclax, etc.…”

Synthesis and in vitro biological activity of chalcone derivatives as potential antiparasitic agents

“…m-NO 2 , and p-Cl substituted derivatives showed the best antiparasitic activities, while ortho Fig. 1 Biological activities of different chalcone derivatives [36,[43][44][45] substitution, and derivatives with electron donating substituents were generally not active.…”

“…Chalcones, also known as 1,3-diphenyl-2-propene, are intermediates in the synthesis of several biologically important classes of compounds such as flavones, pyrimidines, pyrazoles, indoles [35]. In several cases, chalcone and its derivatives have been identified from numerous medicinal plants like Dracaena cinnabari, Medicago sativa, and Angelica keiskei [36]. There have been reports of chalcones exhibiting a variety of biological and pharmacological properties such as antiinflammatory, analgesic, anti-oxidant, anti-bacterial, antifungal, anti-viral, anti-tumor, and anti-parasitic activity [37][38][39][40].…”

Recent developments on microwave-assisted organic synthesis of nitrogen- and oxygen-containing preferred heterocyclic scaffolds

“…51,52 Quinoline serves as a precursor for numerous derivatives with diverse properties. Many quinoline derivatives exhibit potent pharmacological activities, 53 including anti-malarial drugs such as chloroquine 54 and anti-cancer agents such as camptothecin. 55 Its derivatives have been studied for their potential in treating neurodegenerative diseases because they can interact with specific receptors in the brain.…”