Synthesis and antibacterial activity of 4''-O-heteroarylcarbamoyl derivatives of macrolide.
A series of novel 4''-position modified macrolide derivatives has been synthesized via a facile procedure. Their in vitro antibacterial activities against constitutively erythromycin-resistant strains were evaluated. Among the derivatives tested, compound 8a which has 11,12-carbamate and 4''-O-heteroarylcarbamoyl groups was found to have potent activity against most resistant bacteria.
Xu
Peng
P
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China.
Liu
Lu
L
Jin
Zhi-ping
ZP
Wang
Guang-qiang
GQ
Liu
Jian
J
Li
Yun
Y
Lei
Ping-sheng
PS
D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002219:Carbamates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D017291:Clarithromycin / Q000737:chemistry*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D013293:Enterococcus faecalis / Q000378:metabolism; D004917:Erythromycin / Q000138:chemical synthesis* / Q000494:pharmacology; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D011500:Protein Synthesis Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D002219:Carbamates; D018942:Macrolides; D011500:Protein Synthesis Inhibitors; D004917:Erythromycin; D017291:Clarithromycin