High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv - 22/08/11

Doi : 10.1016/j.tube.2009.05.008

Subramaniam Ananthan ^a,^{^{d
Tel.: +1 205 581 2822; fax: +1 205 581 2726.}} , Ellen R. Faaleolea ^b,^{^{o
Tel.: +1 301 694 3232x282; fax: +1 301 694 7223.}} , Robert C. Goldman ^c,^{^{q
Present address: 6610 Rockledge Drive, Room 5083, MSC 6603, Bethesda, MD 20817, USA. +1 301 496 8424; fax: +1 301 451 5481.}} , Judith V. Hobrath ^a,^{^{e
Tel.: +1 205 581 2761.}} , Cecil D. Kwong ^a,^{^{f
Tel.: +1 205 581 2746.}} , Barbara E. Laughon ^c,^{^{r
Present address: 6610 Rockledge Drive, Room 4207, Bethesda, MD 20892 USA. Tel.: +1 301 402 0138.}} , Joseph A. Maddry ^a,^{^{g
Tel.: +1 205 581 2748.}} , Alka Mehta ^a,^{^{h
Tel.: +1 205 581 2111.}} , Lynn Rasmussen ^a,^{^{i
Tel.: +1 205 581 2259.}} , Robert C. Reynolds ^a,^{^{j
Tel.: +1 205 581 2454.}} , John A. Secrist ^a,^⁎ , Nice Shindo ^a,^{^{k
Tel.: +1 205 581 2709.}} , Dustin N. Showe ^b,^{^{p
Tel.: +1 301 694 3232x283.}} , Melinda I. Sosa ^a,^{^{l
Tel.: +1 205 581 2440.}} , William J. Suling ^a,^{^{m
Tel.: +1 205 581 2558.}} , E. Lucile White ^a,^{^{n
Tel.: +1 205 581 2344.}}
^a Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA
^b Southern Research Institute, 431 Aviation Way, Frederick, MD 21701, USA
^c DHHS/NIH/NIAID/Division of Acquired Immunodeficiency Syndrome, Therapeutic Research Program, Complications and Coinfections Branch, USA

Corresponding author. Tel.: +1 205 581 2442; fax: +1 205 581 2726.

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.

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Keywords : TAACF, Antitubercular, High-throughput screening methods, Medicinal chemistry analysis, Medicinally relevant chemical library

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Vol 89 - N° 5

P. 334-353 - septembre 2009 Retour au numéro

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Discovery and validation of new antitubercular compounds as potential drug leads and probes
Robert C. Goldman, Barbara E. Laughon

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Antituberculosis activity of the molecular libraries screening center network library
Joseph A. Maddry, Subramaniam Ananthan, Robert C. Goldman, Judith V. Hobrath, Cecil D. Kwong, Clinton Maddox, Lynn Rasmussen, Robert C. Reynolds, John A. Secrist, Melinda I. Sosa, E. Lucile White, Wei Zhang

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High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv - 22/08/11

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