1. Synthesis and antibacterial activities of acylide derivatives bearing an aryl-tetrazolyl chain.
- Author
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Shan LX, Sun PH, Guo BQ, Xu XJ, Li ZQ, Sun JZ, Zhou SF, and Chen WM
- Subjects
- Anti-Bacterial Agents chemistry, Dose-Response Relationship, Drug, Macrolides chemical synthesis, Macrolides chemistry, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship, Tetrazoles chemical synthesis, Tetrazoles chemistry, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents pharmacology, Escherichia coli drug effects, Macrolides pharmacology, Pseudomonas aeruginosa drug effects, Streptococcus drug effects, Tetrazoles pharmacology
- Abstract
Seventeen acylides bearing an aryl-tetrazolyl alkyl-substituted side chain were synthesized, starting from clarithromycin, via several reactions including hydrolysis, acetylating, esterification, carbamylation, and Michael addition. The structures of all new compounds were confirmed by (1)H nuclear magnetic resonance spectroscopy, (13)C nuclear magnetic resonance spectroscopy, and mass spectrometry. All these synthesized acylides were evaluated for in vitro antimicrobial activities against gram-positive pathogens (Staphylococcus aureus, Staphylococcus epidermidis) and gram-negative pathogens (Pseudomonas aeruginosa, Escherichia coli), using the broth microdilution method. Results showed that compounds 10 e, 10 f, 10 g, 10 h, 10 o have good antibacterial activities.
- Published
- 2014
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