Title:Novel S-Mercaptotriazolebenzothiazole-Based Derivatives as Antimicrobial
Agents: Design, Synthesis, and In Vitro Evaluation
Volume: 19
Issue: 10
Author(s): Alaa M. Alqahtani*, Asmaa G. Safi El-Din, Randa Abdou, Ali H. Amin, Hany H. Arab and Ahmed H. Abdelazeem*
Affiliation:
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia
- Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt
- Department of Pharmacy, College of Pharmacy, Riyadh Elm University, Riyadh 11681, Saudi Arabia
Keywords:
Mercaptotriazolebenzothiazole, benzothiazolotriazole, antimicrobial, antibacterial, antifungal, resistance.
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.
