Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety

被引：15

作者：

Shang, Ruofeng ^{[1
]}

Wang, Shengyu ^{[2
]}

Xu, Ximing ^{[3
]}

Yi, Yunpeng ^{[1
]}

Guo, Wenzhu ^{[1
]}

YuLiu ^{[1
]}

Liang, Jianping ^{[1
]}

机构：

[1] Chinese Acad Agr Sci, Lanzhou Inst Anim Sci & Vet Pharmaceut Sci, Key Lab New Anim Drug Project Gansu Prov, Key Lab Vet Pharmacceut Dev,Minist Agr, Lanzhou, Gansu, Peoples R China

[2] Univ Hosp Gansu Tradit Chinese Med, Lanzhou, Gansu, Peoples R China

[3] Univ Paris Diderot, Sorbonne Paris Cite, CNRS, Unite Biol Fonct & Adaptat, Paris, France

来源：

PLOS ONE | 2013年 / 8卷 / 12期

关键词：

ANTIBACTERIAL ACTIVITY; ANTIMICROBIAL ACTIVITY; ANTIBIOTICS; BINDING; CHEMISTRY; COMPLEX; FIT;

D O I：

10.1371/journal.pone.0082595

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These pleuromutilin derivatives with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae. Compound 5b showed the highest antibacterial activities and even exceeded tiamulin. Moreover, the docking experiments provided information about the binding model between the synthesized compounds and peptidyl transferase center (PTC) of 23S rRNA.

引用

页数：10

共 32 条

[1]

Arigoni D., 1962, GAZZ CHIM ITAL, V92, P884

[2]

BIRCH A J., 1963, Chemical Indian Journal, V14, P374

[3] Resistance to the peptidyl transferase inhibitor tiamulin caused by mutation of ribosomal protein L3 [J].