High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv

被引：238

作者：

Ananthan, Subramaniam ^{[1
]}

Faaleolea, Ellen R. ^{[2
]}

Goldman, Robert C. ^{[3
]}

Hobrath, Judith V. ^{[1
]}

Kwong, Cecil D. ^{[1
]}

Laughon, Barbara E. ^{[3
]}

Maddry, Joseph A. ^{[1
]}

Mehta, Alka ^{[1
]}

Rasmussen, Lynn ^{[1
]}

Reynolds, Robert C. ^{[1
]}

Secrist, John A., III ^{[1
]}

Shindo, Nice ^{[1
]}

Showe, Dustin N. ^{[2
]}

Sosa, Melinda I. ^{[1
]}

Suling, William J. ^{[1
]}

White, E. Lucile ^{[1
]}

机构：

[1] So Res Inst, Birmingham, AL 35205 USA

[2] So Res Inst, Frederick, MD 21701 USA

[3] NIAID, DHHS, NIH,Therapeut Res Program,Complicat & Coinfect Br, Div Acquired Immunodeficiency Syndrome, Bethesda, MD USA

来源：

TUBERCULOSIS | 2009年 / 89卷 / 05期

关键词：

TAACF; Antitubercular; High-throughput screening methods; Medicinal chemistry analysis; Medicinally relevant chemical library; DRUG-RESISTANT TUBERCULOSIS; RING-SUBSTITUTED QUINOLINES; MEFLOQUINE-BASED LIGANDS; CELL-WALL BIOSYNTHESIS; PLATE-BASED SCREEN; MULTIDRUG-RESISTANT; IN-VITRO; ANTIMYCOBACTERIAL ACTIVITY; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION;

D O I：

10.1016/j.tube.2009.05.008

中图分类号：

R392 [医学免疫学]; Q939.91 [免疫学];

学科分类号：

100102 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：334 / 353

页数：20

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