Synthesis of pyrazolo-1,2,4-triazolo[4,3-a]quinoxalines as antimicrobial agents with potential inhibition of DHPS enzyme
Aim: The development of a new class of antimicrobial agents is the optimal lifeline to scrap the escalating jeopardy of drug resistance. Experimental: This study aims to design and synthesize a series of pyrazolo-1,2,4-triazolo[4,3-a]quinoxalines, to develop agents having antimicrobial activity through potential inhibition of dihyropteroate synthase enzyme. The target compounds have been evaluated for their in-vitro antimicrobial activity. Results & discussion: Compounds 5b, 5c were equipotent (minimal inhibitory concentration = 12.5 μg/ml) to ampicillin. The docking patterns of 5b and 5c demonstrated that both fit into Bacillus Anthracis dihydropteroate synthase pterin and p-amino benzoic acid-binding pockets. Moreover, their physicochemical properties and pharmacokinetic profiles recommend that they can be considered drug-like candidates. The results highlight some significant information for the future design of lead compounds as antimicrobial agents.
Faculty of Applied Health Sciences Technology
Life Sciences, Pharmacology, Toxicology, Pharmaceutical Science
Indexed in Scopus
Indexed in Web Of Science
antibacterial activity, antibacterial efficiency, antifungal activity, dihydropteroate synthase, docking, enzyme inhibition, pharmacokinetics, physicochemical properties, pyrazole, synthesis, triazoloquinoxalines
El-Attar, Maryam A.Z.; Elbayaa, Rasha Y.; Shaaban, Omaima G.; Habib, Nargues S.; Abdel Wahab, Abeer E.; Abdelwahab, Ibrahim A.; and El-Hawash, Soad A.M., "Synthesis of pyrazolo-1,2,4-triazolo[4,3-a]quinoxalines as antimicrobial agents with potential inhibition of DHPS enzyme" (2018). Faculty of Applied Health Sciences Technology. 96.