Abstract
Background: The search for novel antimicrobial agents effective against the emerging resistant pathogenic microorganisms to the currently used drugs is a substantial need. Herein, a novel series of compounds bearing a benzothiazolotriazole scaffold was synthesized and evaluated as potential antimicrobial agents against a panel of gram +ve, gram -ve bacteria, and fungi species.
Methods: The new compounds were synthesized via hybridization between the benzothiazolotriazole scaffold and thiadiazole ring or various substituted aromatic moieties using the tethering technique in drug discovery.
Results: The in vitro results revealed that these compounds have significant antifungal activity rather than antibacterial potential due to their high similarity with tricyclazole. Compound 7b bearing bromo-phenyl moiety was the most potent derivative with an MIC value of 8 μg/mL against Candida albicans and Penicillium chrysogenum.
Conclusion: Collectively, benzothiazolotriazole-based derivatives are good antifungal leads and should be further actively pursued to expand treatment options for systemic and topical fungal infections.
Keywords: Mercaptotriazolebenzothiazole, benzothiazolotriazole, antimicrobial, antibacterial, antifungal, resistance.
Graphical Abstract
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