Synthesis, antimicrobial activity, and biofilm inhibition studies of 1,2,3-triazole-containing 2,3-dihydrothiazole

Abstract

The newly synthesized 1,2,3-triazole-thiazole hybrids were first evaluated for their antimicrobial activity against different microbial strains. Most of it showed a marked selectivity against Gram-positive and Gram-negative bacterial strains. The MIC assay was then assessed; for S. aureus, 4a was equipotent to the reference neomycin, while 3a, 3b, and 8b were 2-fold lower. For E. coli, compounds 3a, 4a, and 8c were equipotent to neomycin, while 5a was 8-fold higher, and 8d was 2-fold higher. Most of tested compounds showed superiority to the reference drug against C. albicans; 8a and 8e showed MIC value of 16-fold higher than neomycin, while 3a was 8-fold higher. Also, 3b and 8f were 4-fold higher; 8d was 2-fold higher, while 5a was equipotent to neomycin against the same microbe. Further biofilm formation inhibition assay was conducted to the most active compounds, 5a was the most active against the three types of bacterial strains.

Graphical Abstract

Keywords:

• Antimicrobial activity
• biofilm inhibition
• dihydrothiazole
• triazole

Disclosure statement

There are no conflicts to declare.

Author contributions

Ashraf A. Sediek: Conceptualization, Investigation, Supervision, Methodology, Writing-original draft.

Ahmed Younis: Methodology, Investigation, Writing-review and editing.

Asmaa F. Kassem: Methodology, Investigation, Writing-review and editing.

Mohamed S. Abdel-Aziz: Biological evaluation.