4.5 Article

Green synthesis of novel antifungal 1,2,4-triazoles effective against γ-irradiated Candida parapsilosis

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ARCHIV DER PHARMAZIE
卷 355, 期 1, 页码 -

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.202100287

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antibacterial activity; antifungal activity; antimicrobial activity; rational drug design; triazoles

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This study successfully synthesized 11 novel triazole derivatives using water as a green solvent, and found that one of the derivatives, compound 6, exhibited promising antimicrobial activity against both fungal and bacterial strains, as well as inhibitory effects on specific enzymes, without displaying cytotoxicity.
This study reports the green synthesis of 11 novel 3-substituted-4-amino-5-mercapto-1,2,4-triazole derivatives using water as a readily available nontoxic solvent. Evaluation of their antimicrobial potential against several clinical pathogenic microorganisms was carried out. The newly synthesized cysteine derivative 6 showed promising antifungal activity against both gamma-irradiated and nonirradiated Candida parapsilosis 216, with the lowest MIC (minimum inhibitory concentration) value of 3.125 mu g/ml, probably through inhibition of 14 alpha-demethylase. In addition, compound 6 showed complete inhibition of gelatinase, a virulence enzyme of C. parapsilosis. Also, scanning electron microscopy was carried out. Interestingly, compound 6 acted as a dual agent as it also showed good antibacterial activity against strains of Gram-positive bacteria used in the study. The synthesized compounds showed no cytotoxicity.

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