Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 33, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127746
Keywords
Molecular hybridization; Click chemistry; Triazole-thiazole hybrids; Antimicrobial activity; Antibiofilm activity
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Funding
- ICMR-National Institute for Research in Environmental Health (NIREH), Bhopal
- Ministry of Human Resource Development (MHRD)
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A new series of triazole-thiazole hybrids were synthesized and evaluated for their in vitro antimicrobial activity, showing promising inhibitory effects against bacterial and Candida strains. Compounds 8i, 8k, and 8l demonstrated significant biofilm inhibitory activity against Bacillus subtilis and Staphylococcus aureus.
A new series of triazole-thiazole hybrids were designed, synthesized by the Multi-component reaction approach and evaluated in vitro antimicrobial activity. Most of the tested series of compounds exhibited promising inhibitory activity against the bacterial strains with values in the range of 2.8 to 15.7 mu M. The compounds 8i-8l and 8r showed potential-Candida activity against various Candida strains with spectrum values in the range 5.9-14.2 mu M. Further, anti-biofilm and toxicity profiles for the potent compounds were also tested, and it was observed that the compounds 8i, 8k, and 8l were found to inhibit the biofilm formation with IC50 values of 6.6, 16.6 and 15.9 mu M, respectively against Bacillus subtilis MTCC 121. Besides, 8k and 8l also displayed promising biofilm formation inhibitory activity towards Staphylococcus aureus MTCC 96 with IC50 values of 13.5 and 12.0 mu M respectively. In summary, the activity results has emphasized the compounds 8k and 8l as potential leads for further development of antibacterial, anti-Candida, and anti-biofilm agents.
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