Synthesis and Biological Evaluation of Novel Thioether Pleuromutilin Derivatives

文献类型： 外文期刊

第一作者： Mu, Shuhua

作者： Mu, Shuhua;Zhang, Yue;Mu, Shuhua;Liu, Huixian;Zhang, Lifang;Wang, Xiaoyang;Xue, Feiqun

作者机构：

关键词： pleuromutilin derivative;antibacterial activity;acylation reaction;2-aminothiazol

期刊名称：BIOLOGICAL & PHARMACEUTICAL BULLETIN （ 影响因子：2.233； 五年影响因子：2.309 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： To develop new pleuromutilin derivatives as veterinary antibiotic medicines, we designed and synthesized a series of new thioether pleuromutilin derivatives possessing acylthiazolyl moiety based on previously designed derivatives. The antibacterial properties of the prepared pleuromutilin derivatives were assessed in vitro by the broth dilution method against five kinds of bacteria and the mycoplasma Mycoplasma gallisepticum (MG). All of the tested compounds displayed moderate to good antibacterial activity to methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-sensitive Staphylococcus epidermidis (MSSE), methicillin-resistant S. aureus (MRSA), Streptococcus agalactiae (S. aga) and MG. However, the activity to Pyogeniccoccus (Pyogens) was generally poor. Compounds 13i and 1 showed potent antibacterial activity against MSSE and MRSA which are better than that of valnemulin. The structural modification for pleuromutilin affected the antibacterial activity. Amino substituents in the benzene ring can effectively improve activity. Compared with the analogue 13a that possesses unsubstitution benzoyl group, the nitro, methoxy, hydroxy and dichloro substituent contributed little to antibacterial activity. Increasing a methylene between benzene moiety and carbonyl group decreased the bioactivity of derivative. The analogues that obtained by the reaction of amino acids and intermediate 9 showed moderate activity.

分类号： R9

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