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Synthesis and biological evaluation of new 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives
- Source :
- Research on Chemical Intermediates. 44:1247-1260
- Publication Year :
- 2017
- Publisher :
- Springer Science and Business Media LLC, 2017.
-
Abstract
- A series of 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives (8a–p) have been synthesized. The structure of the newly synthesized compounds was determined by spectral analysis. The title compounds were screened for their preliminary antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB, ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Further, the synthesized compounds were screened for antimicrobial activity against standard Gram-negative bacteria Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059) and Gram-positive bacteria Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162). Among all the synthesized compounds, 8a–c, f–h, m exhibited good activity against dormant M. bovis BCG strain. Compounds 8h, j exhibited good activity against all tested bacterial strains. All active compounds were screened for cytotoxicity and found inactive. Their high potency and promising antimycobacterial activity suggest that these compounds could serve as good leads for further optimization and development.
- Subjects :
- 1,2,3-Triazole
biology
010405 organic chemistry
Stereochemistry
medicine.drug_class
General Chemistry
Bacillus subtilis
medicine.disease_cause
biology.organism_classification
Antimicrobial
Antimycobacterial
01 natural sciences
0104 chemical sciences
Mycobacterium tuberculosis
010404 medicinal & biomolecular chemistry
chemistry.chemical_compound
chemistry
medicine
Thiazole
Antibacterial activity
Escherichia coli
Subjects
Details
- ISSN :
- 15685675 and 09226168
- Volume :
- 44
- Database :
- OpenAIRE
- Journal :
- Research on Chemical Intermediates
- Accession number :
- edsair.doi...........f68a7eceb7eede891ad8a9bc0762c379
- Full Text :
- https://doi.org/10.1007/s11164-017-3164-4