期刊
MEDICINAL CHEMISTRY RESEARCH
卷 23, 期 6, 页码 2995-3004出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-013-0882-z
关键词
1,4-Disubstituted 1,2,3-bistriazoles; Click chemistry; Antimicrobial activity; Docking simulation
资金
- University Grants Commission, New Delhi
A small library of amino acid-linked 1,4-disubstituted 1,2,3-bistriazole conjugates has been synthesized from the N-protected l-amino acids propargyl esters through one-pot click reaction. All the newly synthesized compounds were tested in vitro for antimicrobial activity against Gram-positive (Staphylococcus aureus, Bacillus subtilis), Gram-negative (Escherichia coli) bacteria and fungi (Candida albicans, Aspergillus niger). The antibacterial evaluation data indicated that compounds 3c, 3h, 5a, 5b, 5c, 5d, 5e, 5g, and 5h exhibited comparable activity to standard ciprofloxacin. However, the bistriazoles 3b, 3c, 3e, 3f, and 3g showed good antifungal activity than others against both fungi. Further, docking simulation of the two most active compounds 5c against S. aureus tyrosyl tRNA synthetase and 5h into E. coli topoisomerase II DNA Gyrase B, respectively, was also performed.
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