Natural products - The future scaffolds for novel antibiotics?

被引：253

作者：

Butler, MS ^{[1
]}

Buss, AD ^{[1
]}

机构：

[1] Merlion Pharmaceut, Singapore 117528, Singapore

来源：

BIOCHEMICAL PHARMACOLOGY | 2006年 / 71卷 / 07期

关键词：

natural product; clinical trial; template; antibacterial; antibiotic; assay;

D O I：

10.1016/j.bcp.2005.10.012

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Natural products have played a pivotal role in antibiotic drug discovery with most antibacterial drugs being derived from a natural product or natural product lead. However, the rapid onset of resistance to most antibacterial drugs diminishes their effectiveness considerably and necessitates a constant supply of new antibiotics for effective treatment of infections. The natural product templates of actinonin, pleuromutilin, ramoplanin and tiacumicin B, which are compounds undergoing clinical evaluation, represent templates not found in currently marketed antibacterial drugs. In addition, the new templates present in the recently discovered lead antibacterials arylomycin, GE23077, mannopeptimycin, muraymycin/caprazamycin, nocathiacin and ECO-0501, are discussed. Despite extensive efforts to identify antibiotic leads from molecular targets, only the peptide deformylase inhibitor LBM-415 is currently in clinical trials. It is proposed that new antibacterial assays which combine cell-based screening with molecular targets could offer better prospects for lead discovery. (c) 2005 Elsevier Inc. All rights reserved.

引用

页码：919 / 929

页数：11

共 92 条

[81] INVITRO AND INVIVO EVALUATION OF TIACUMICIN-B AND TIACUMICIN-C AGAINST CLOSTRIDIUM-DIFFICILE [J].