Synthesis of Amide Core Based New 5‐methyl‐2‐(2 <i>H</i> ‐1,2,3‐triazol‐2‐yl)benzamide Scaffolds As Antifungal, Antimicrobial Agents, and Molecular Docking Study
Abstract A new series of new 5‐methyl‐2‐(2 H ‐1,2,3‐triazol‐2‐yl)benzamide was successfully designed and synthesized by acid amine coupling reaction of 5‐methyl‐2‐(2H‐1,2,3‐triazol‐2‐yl)benzoic acid and different types of aliphatic and aromatic amines. The compounds were characterized by 1 H NMR, 13 C NMR, FT‐IR and mass spectra. The synthesized scaffolds (H1‐H20) were evaluated for its antifungal and antibacterial activity in vitro against C. albicans (Candida albicans), A. clavatus (Aspergillus clavatus), A. niger (Aspergillus Niger), E. coli (Escherichia coli), P. aeruginosa (Pseudomonas Aeruginosa), S. aureus (Staphylococcus Aureus) , and S. pyogenes (Streptococcus Pyogenus) . Compounds H3 , H7 , H9 , H13 , H14 , H17 , and H19 were most effective ( MIC 250 µg/mL ) against C. albicans compared to standard drug griseofulvin ( MIC 500 µg/mL ). The antibacterial activity of all synthesized 1,2,3‐triazoles scaffolds were good to moderate compared to ciprofloxacin and chloramphenicol standard drugs. Moreover, in silico molecular docking study, the compounds with highest potential activity examine. The result showed strong receptor site binding affinity and indicated promising antifungal and antibacterial potential.
Authors
- Dhanaji P. Rajani
- Vaishali Chaudhari
- Ravindra Kulkarni
- V. B. Patil (ORCID: https://orcid.org/0000-0001-8729-4176)
- Hanuman Narode (ORCID: https://orcid.org/0009-0007-5287-5991)
- Shally Rana (ORCID: https://orcid.org/0000-0001-6414-5178)
- Rajesh S. Bhosale (ORCID: https://orcid.org/0000-0002-8422-6941)
- Manoj Gayke
- Rutuja Gunjate
Institutions
- Indrashil University (IN)
- Ganpat University (IN)
- Savitribai Phule Pune University (IN)
Publication Details
- Journal
- ChemistrySelect
- Published
- 2025-04-01
- DOI
- https://doi.org/10.1002/slct.202404415
- Citations
- 1
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.94
Funders
- Department of Science and Technology, Ministry of Science and Technology, India