Design,synthesis and antibacterial activity of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain |
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Authors: | Chen-Yu Ling Yun-Liang Tao Wen-Jing Chu Hui Wang Hai-Dong Wang Yu-She Yang |
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Institution: | a. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
b. School of Petrochemical Engineering, Changzhou University, Changzhou 213164, China;
c. Department of Microbiology, China Pharmaceutical University, Nanjing 210009, China |
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Abstract: | 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. |
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Keywords: | Multi-drug resistant bacteria Pleuromutilin 4H-Pyran-4-one Antibacterial activity |
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