Synthesis and evaluation of novel pleuromutilin derivatives with a substituted pyrimidine moiety.
Basic Information
ID: ALA3608216
Journal: Eur J Med Chem
Title: Synthesis and evaluation of novel pleuromutilin derivatives with a substituted pyrimidine moiety.
Authors: Yi Y, Yang G, Zhang C, Chen J, Liang J, Shang R.
Abstract: A series of novel pleuromutilin derivatives possessing 6-hydroxy pyrimidine moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphylococcus epidermidis (MRSE), Bacillus subtilis (B. subtilis), and Escherichia coli (E. coli) were tested by the agar dilution method. The majority of the screened compounds displayed potent activities. Compounds 3 and 6a were found to be the most active antibacterial agents against MRSA and MRSE. Moreover, in the vivo experiment, compound 6a showed comparable antibacterial activity to that of tiamulin, with ED50 of 5.47 mg/kg body weight against MRSA.
CiteXplore: 26134552
DOI: 10.1016/j.ejmech.2015.06.034
Patent ID: ┄