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

作     者：Chen-Yu Ling Yun-Liang Tao Wen-Jing Chu Hui Wang Hai-Dong Wang Yu-She Yang 

作者机构：State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences School of Petrochemical Engineering Changzhou University Department of Microbiology China Pharmaceutical University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2016年第27卷第2期

页      码：235-240页

摘      要：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 12 a, 12 d, 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.

主 题 词：Multi-drug resistant bacteria Pleuromutilin 4H-Pyran-4-one Antibacterial activity 

学科分类：1007[医学-药学类] 081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 070303[070303] 0703[理学-化学类] 10[医学] 

核心收录：

D　O　I：10.1016/j.cclet.2015.09.019

馆 藏 号：203846273...