کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1399180 | 1501153 | 2013 | 8 صفحه PDF | دانلود رایگان |
A series of novel pleuromutilin derivatives possessing thioether moiety has been synthesized via acylation reaction under mild conditions. Their in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae were tested by agar dilution method and Oxford cup assay. Among the 17 compounds screened, 14-O-[(4-methoxybenzamide-2- methylpropane-2-yl) thioacetate] mutilin 4i, 14-O-[(2-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5a and 14-O-[(4-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5c were resulted as most active antibacterial agents.
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► A series of novel pleuromutilin derivatives were synthesized under very mild conditions.
► Synthesized compounds were evaluated for their antibacterial activity by agar dilution method and Oxford cup assay.
► Most of these compounds possess antibacterial activity.
► Three compounds 4i, 5a, 5c showed excellent antibacterial activity.
Journal: European Journal of Medicinal Chemistry - Volume 63, May 2013, Pages 231–238