Abstract
Platensimycin, an active metabolite of Streptomyces platensis, was initially discovered by a combination of RNA interferin induced gene-silencing and library screening to microbial extracts. Platensimycin selectively inhibits β- ketoacyl-acyl carrier protein (ACP) synthase II (FabF) that is recognized as an effective broad-spectrum antibiotic against drug-resistant microorganism strains. Its novel scaffold and extraordinary antibacterial activity have drawn great attentions in recent years. So far, a number of synthetic strategies have been explored for the total synthesis of platensimycin. Moreover, many analogues have been investigated in terms of structure-activity relationships (SAR). This review provides a detailed overview of updated studies on platensimycin, focusing on various total and formal synthetic strategies, development of analogues, and the structure-activity relationships.
Keywords: Platensimycin, FabF, antibiotic, discovery, platencin, total synthetic strategies, analogues, SAR
Current Medicinal Chemistry
Title: Recent Advances on Platensimycin: A Potential Antimicrobial Agent
Volume: 17 Issue: 12
Author(s): Xiaoyun Lu and Qidong You
Affiliation:
Keywords: Platensimycin, FabF, antibiotic, discovery, platencin, total synthetic strategies, analogues, SAR
Abstract: Platensimycin, an active metabolite of Streptomyces platensis, was initially discovered by a combination of RNA interferin induced gene-silencing and library screening to microbial extracts. Platensimycin selectively inhibits β- ketoacyl-acyl carrier protein (ACP) synthase II (FabF) that is recognized as an effective broad-spectrum antibiotic against drug-resistant microorganism strains. Its novel scaffold and extraordinary antibacterial activity have drawn great attentions in recent years. So far, a number of synthetic strategies have been explored for the total synthesis of platensimycin. Moreover, many analogues have been investigated in terms of structure-activity relationships (SAR). This review provides a detailed overview of updated studies on platensimycin, focusing on various total and formal synthetic strategies, development of analogues, and the structure-activity relationships.
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Cite this article as:
Lu Xiaoyun and You Qidong, Recent Advances on Platensimycin: A Potential Antimicrobial Agent, Current Medicinal Chemistry 2010; 17 (12) . https://dx.doi.org/10.2174/092986710790827852
DOI https://dx.doi.org/10.2174/092986710790827852 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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