Synthesis, antibacterial activity, and CoMFA study of new 1,2,3-triazolyl 7-carboxamidodesacetoxy cephalosporanic acid derivatives

被引：0
作者：
Maryam Mohebbi
Peyman Salehi
Morteza Bararjanian
Atousa Aliahmadi
Reihaneh Safavi-Sohi
Jahan B. Ghasemi
机构：
[1] Shahid Beheshti University,Department of Phytochemistry, Medicinal Plants and Drugs Research Institute
[2] Shahid Beheshti University,Department of Biology, Medicinal Plants and Drugs Research Institute
[3] K. N. Toosi University of Technology,Department of Chemistry, Faculty of Sciences
来源：
Medicinal Chemistry Research | 2014年 / 23卷
关键词：
Cephalosporins; Click chemistry; CoMFA study; Antibacterial; Synergistic effect;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
New derivatives of 1,2,3-triazolyl 7-carboxamidodesacetoxy cephalosporanic acid were synthesized using alkyne-azide 1,3-dipolar cycloaddition. The synthesized compounds were evaluated for their antibacterial activity against a collection of Gram-positive and Gram-negative bacteria and also in synergy with cefixime and cephalexin. Some compounds inhibited vancomycin-resistant strain of Enterococcus faecium (MIC = 8 µg/mL) and in the synergy experiments compounds 13a, 13f, and 13g decreased the level of MIC against an ESBL strain of Klebsiella pneumonia. A comparative molecular field analysis has been carried out, and the effect of substituents on the antibacterial activities of the synthesized compounds was explained.
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页码：4531 / 4541
页数：10
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