Title

Synthesis of pyrazolo-1,2,4-triazolo[4,3-a]quinoxalines as antimicrobial agents with potential inhibition of DHPS enzyme

Document Type

Article

Abstract

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.

Publication Date

9-1-2018

Faculty

Faculty of Applied Health Sciences Technology

Subject Area

Life Sciences, Pharmacology, Toxicology, Pharmaceutical Science

Indexed in Scopus

yes

Indexed in Web Of Science

yes

DOI

https://doi.org/10.4155/fmc-2018-0082

Volume

10

Keywords

antibacterial activity, antibacterial efficiency, antifungal activity, dihydropteroate synthase, docking, enzyme inhibition, pharmacokinetics, physicochemical properties, pyrazole, synthesis, triazoloquinoxalines

ISSN

17568919

eISSN

17568927

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