کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1257024 | 971541 | 2016 | 6 صفحه PDF | دانلود رایگان |

A series of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain have been designed and synthesized. In vitro antibacterial activity evaluation showed that most of the derivatives exhibited potent antibacterial activity against drug resistant Gram-positive strains. Compounds 12a, 12d, and 28 are the most active derivatives in this series, displaying activity comparable to that of retapamulin and BC-3781. As the metabolic stability of this series is not satisfactory, further modifications are going on to improve their pharmacokinetic profile.
A series of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain have been synthesized. Structure–activity relationship study showed that 4H-pyran-4-one moiety is favored over pyridin-4-one. Among the series, compounds 12a, 12d and 28 exhibited excellent antibacterial activity against selected Gram-positive strains including MRSA, MRSE, and PRSP.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 27, Issue 2, February 2016, Pages 235–240