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Letters in Drug Design & Discovery

Author(s): Alaa M. Alqahtani*, Asmaa G. Safi El-Din, Randa Abdou, Ali H. Amin, Hany H. Arab and Ahmed H. Abdelazeem*

DOI: 10.2174/1570180819666220301154851

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Novel S-Mercaptotriazolebenzothiazole-Based Derivatives as Antimicrobial Agents: Design, Synthesis, and In Vitro Evaluation

Page: [925 - 937] Pages: 13

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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.

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