High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv

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• 作者：Subramaniam Ananthan ; Ellen R. Faaleolea ; Robert C. Goldman ; Judith V. Hobrath ; Cecil D. Kwong ; Barbara E. Laughon ; Joseph A. Maddry ; Alka Mehta ; Lynn Rasmussen ; Robert C. Reynolds ; John A. Secrist II
• 关键词：TAACF ; Antitubercular ; High-throughput screening methods ; Medicinal chemistry analysis ; Medicinally relevant chemical library
• 刊名：Tuberculosis
• 出版年：2009
• 出版时间：September 2009
• 年：2009
• 卷：89
• 期：5
• 页码：334-353
• 全文大小：1030 K

文摘

Summary

There is an urgent need for the discovery and development of new antitubercular agents that target new biochemical pathways and treat drug resistant forms of the disease. One approach to addressing this need is through high-throughput screening of medicinally relevant libraries against the whole bacterium in order to discover a variety of new, active scaffolds that will stimulate new biological research and drug discovery. Through the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (www.taacf.org), a large, medicinally relevant chemical library was screened against M. tuberculosis strain H37Rv. The screening methods and a medicinal chemistry analysis of the results are reported herein.