Literature DB >> 33333162

1,2,3-triazole-thiazole hybrids: Synthesis, in vitro antimicrobial activity and antibiofilm studies.

Ramesh Gondru1, Sirisha Kanugala2, Sneha Raj3, C Ganesh Kumar2, Mukesh Pasupuleti4, Janardhan Banothu5, Rajitha Bavantula6.   

Abstract

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 µM. The compounds 8i-8l and 8r showed potential-Candida activity against various Candida strains with spectrum values in the range 5.9-14.2 µM. 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 µM, 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 µM 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.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibiofilm activity; Antimicrobial activity; Click chemistry; Molecular hybridization; Triazole-thiazole hybrids

Year:  2020        PMID: 33333162     DOI: 10.1016/j.bmcl.2020.127746

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Urea-thiazole/benzothiazole hybrids with a triazole linker: synthesis, antimicrobial potential, pharmacokinetic profile and in silico mechanistic studies.

Authors:  Nisha Poonia; Kashmiri Lal; Ashwani Kumar; Anil Kumar; Srikanta Sahu; Anurag T K Baidya; Rajnish Kumar
Journal:  Mol Divers       Date:  2021-10-20       Impact factor: 3.364

Review 2.  Bacterial virulence factors: a target for heterocyclic compounds to combat bacterial resistance.

Authors:  Rehab H Abd El-Aleam; Riham F George; Hanan H Georgey; Hamdy M Abdel-Rahman
Journal:  RSC Adv       Date:  2021-11-19       Impact factor: 4.036

Review 3.  3-(Bromoacetyl)coumarins: unraveling their synthesis, chemistry, and applications.

Authors:  Moaz M Abdou; Ahmed Abu-Rayyan; Ahmed G Bedir; S Abdel-Fattah; A M A Omar; Abdullah A Ahmed; El-Sayed I El-Desoky; Eslam A Ghaith
Journal:  RSC Adv       Date:  2021-11-29       Impact factor: 3.361

4.  Design, Synthesis, in vitro and in silico Characterization of 2-Quinolone-L-alaninate-1,2,3-triazoles as Antimicrobial Agents.

Authors:  Oussama Moussaoui; Rajendra Bhadane; Riham Sghyar; Janez Ilaš; El Mestafa El Hadrami; Said Chakroune; Outi M H Salo-Ahen
Journal:  ChemMedChem       Date:  2022-01-27       Impact factor: 3.540

5.  Copper-doped functionalized β-cyclodextrin as an efficient green nanocatalyst for synthesis of 1,2,3-triazoles in water.

Authors:  Mahdieh Tajbakhsh; Mohammad Reza Naimi-Jamal
Journal:  Sci Rep       Date:  2022-03-23       Impact factor: 4.379

  5 in total

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