期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 143, 期 -, 页码 1524-1534出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.10.042
关键词
Quinolone; 1,2,3-Triazole; Conjugate; Antibacterial; QSAR
资金
- National Plan for Science, Technology and Innovation (MAARIFAH) - King Abdulaziz City for Science and Technology - the Kingdom of Saudi Arabia [12-ADV2732-03]
A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10-15, 17-19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17-19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1-3. 2D-QSAR modeling supports the observed biological properties. (C) 2017 Elsevier Masson SAS. All rights reserved.
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