Citation: Chen-Yu Ling, Yun-Liang Tao, Wen-Jing Chu, Hui Wang, Hai-Dong Wang, Yu-She Yang. 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[J]. Chinese Chemical Letters, ;2016, 27(02): 235-240. doi: 10.1016/j.cclet.2015.09.019 shu

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

a.
a. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
b.
b. School of Petrochemical Engineering, Changzhou University, Changzhou 213164, China;
c.
c. Department of Microbiology, China Pharmaceutical University, Nanjing 210009, China

Corresponding author: Hai-Dong Wang, Yu-She Yang,
Received Date: 10 March 2015
Available Online: 15 June 2015

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.
- Multi-drug resistant bacteria,
- Pleuromutilin,
- 4H-Pyran-4-one,
- Antibacterial activity
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