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Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates

Reem I. Al-Wabli, Mona A. Alsulami, Sarah I. Bukhari, Nadine Moubayed, Maha S. Almutairi, Mohamed I. Attia

2021Molecules36 citationsDOIOpen Access PDF

Abstract

The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates 6a-u was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans.

Topics & Concepts

AntimicrobialCandida albicansMinimum inhibitory concentrationCandida tropicalisMicrobiologyIn vitroChemistryIndole testTriazoleAntibacterial activityCombinatorial chemistryStereochemistryBiologyBacteriaBiochemistryOrganic chemistryGeneticsSynthesis and Biological EvaluationClick Chemistry and ApplicationsSynthesis and biological activity
Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates | Litcius