Polycyclic Polyprenylated Acylphloroglucinols: An Emerging Class of Non-Peptide-Based MRSA- and VRE-Active Antibiotics

被引：38

作者：

Guttroff, Claudia ^{[1
]}

Baykal, Aslihan ^{[1
]}

Wang, Huanhuan ^{[2
]}

Popella, Peter ^{[2
]}

Kraus, Frank ^{[1
]}

Biber, Nicole ^{[1
]}

Krauss, Sophia ^{[2
]}

Goetz, Friedrich ^{[2
]}

Plietker, Bernd ^{[1
]}

机构：

[1] Univ Stuttgart, Inst Organ Chem, Pfaffenwaldring 55, D-70569 Stuttgart, Germany

[2] Univ Tubingen, Interfak Inst Mikrobiol & Infekt Med Tubingen IMI, Mikrobielle Genet, Morgenstelle 28, D-72076 Tubingen, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2017年 / 56卷 / 50期

关键词：

antibiotic activity; Gram-positive bacteria; resistance; total synthesis; ST-JOHNS-WORT; RESISTANT STAPHYLOCOCCUS-AUREUS; GRAM-POSITIVE BACTERIA; ENTEROCOCCUS-FAECIUM; VANCOMYCIN-INTERMEDIATE; LEISHMANICIDAL ACTIVITY; ANTIBACTERIAL ACTIVITY; X-RECEPTOR; BENZOPHENONES; DERIVATIVES;

D O I：

10.1002/anie.201707069

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In the past 20 years, peptide-based antibiotics, such as vancomycin, teicoplanin, and daptomycin, have often been considered as second-line antibiotics. However, in recent years, an increasing number of reports on vancomycin resistance in pathogens appeared, which forces researchers to find novel lead structures for potent new antibiotics. Herein, we report the total synthesis of a defined endo-typeB PPAP library and their antibiotic activity against multiresistant S.aureus and various vancomycin-resistant Enterococci. Four new compounds that combine high activities and low cytotoxicity were identified, indicating that the PPAP core might become a new non-peptide-based lead structure in antibiotic research.

引用

页码：15852 / 15856

页数：5