Synthesis of pyrazolo-1,2,4-triazolo[4,3

• Published in: Future medicinal chemistry Vol. 10; no. 18; pp. 2155 - 2175
• Main Authors: Z El-Attar, Maryam A, Elbayaa, Rasha Y, Shaaban, Omaima G, Habib, Nargues S, Abdel Wahab, Abeer E, Abdelwahab, Ibrahim A, M El-Hawash, Soad A
• Format: Journal Article
• Language: English
• Published: Future Science Ltd 01-08-2018; 01-09-2018
• Subjects: antibacterial activity; antibacterial efficiency; antifungal activity; dihydropteroate synthase; docking; enzyme inhibition; pharmacokinetics; physicochemical properties; pyrazole; synthesis; triazoloquinoxalines
• ISSN: 1756-8919; 1756-8927
• DOI: 10.4155/fmc-2018-0082

The development of a new class of antimicrobial agents is the optimal lifeline to scrap the escalating jeopardy of drug resistance.
This study aims to design and synthesize a series of pyrazolo-1,2,4-triazolo[4,3-
]quinoxalines, to develop agents having antimicrobial activity through potential inhibition of dihyropteroate synthase enzyme. The target compounds have been evaluated for their
antimicrobial activity.
Compounds
were equipotent (minimal inhibitory concentration = 12.5 μg/ml) to ampicillin. The docking patterns of
and
demonstrated that both fit into
dihydropteroate synthase pterin and
-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.