High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.
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.
Ananthan
Subramaniam
S
Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA. ananthan@southernresearch.org
Faaleolea
Ellen R
ER
Goldman
Robert C
RC
Hobrath
Judith V
JV
Kwong
Cecil D
CD
Laughon
Barbara E
BE
Maddry
Joseph A
JA
Mehta
Alka
A
Rasmussen
Lynn
L
Reynolds
Robert C
RC
Secrist
John A
JA
Shindo
Nice
N
Showe
Dustin N
DN
Sosa
Melinda I
MI
Suling
William J
WJ
White
E Lucile
EL
D000995:Antitubercular Agents / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007155:Immunologic Factors / Q000494:pharmacology*; D007167:Immunotherapy / Q000379:methods*; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000302:isolation & purification; D054852:Small Molecule Libraries; D014376:Tuberculosis / Q000188:drug therapy* / Q000235:genetics / Q000628:therapy
D000995:Antitubercular Agents; D001426:Bacterial Proteins; D007155:Immunologic Factors; D054852:Small Molecule Libraries