Antituberculosis activity of the molecular libraries screening center network library

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• 作者：Joseph A. Maddry ; Subramaniam Ananthan ; Robert C. Goldman ; Judith V. Hobrath ; Cecil D. Kwong ; Clinton Maddox ; Lynn Rasmussen ; Robert C. Reynolds ; John A. Secrist III ; Melinda I. Sosa ; E. Lucile White
• 关键词：MLSCN ; TAACF ; Antitubercular ; High-throughput screening ; Medicinal chemistry analysis ; Small molecule chemical library ; Tuberculosis
• 刊名：Tuberculosis
• 出版年：2009
• 出版时间：September 2009
• 年：2009
• 卷：89
• 期：5
• 页码：354-363
• 全文大小：729 K

文摘

Summary

There is an urgent need for the discovery and development of new antitubercular agents that target novel biochemical pathways and treat drug-resistant forms of the disease. One approach to addressing this need is through high-throughput screening of drug-like small molecule libraries against the whole bacterium in order to identify a variety of new, active scaffolds that will stimulate additional biological research and drug discovery. Through the Molecular Libraries Screening Center Network, the NIAID Tuberculosis Antimicrobial Acquisition and Coordinating Facility tested a 215,110-compound library against Mycobacterium tuberculosis strain H37Rv. A medicinal chemistry survey of the results from the screening campaign is reported herein.