title: High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.
abstract: 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.
authors.affiliation: Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA. ananthan@southernresearch.org
authors.forename: Subramaniam
authors.initials: S
authors.lastname: Ananthan
authors.forename: Ellen R
authors.initials: ER
authors.lastname: Faaleolea
authors.forename: Robert C
authors.initials: RC
authors.lastname: Goldman
authors.forename: Judith V
authors.initials: JV
authors.lastname: Hobrath
authors.forename: Cecil D
authors.initials: CD
authors.lastname: Kwong
authors.forename: Barbara E
authors.initials: BE
authors.lastname: Laughon
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Maddry
authors.forename: Alka
authors.initials: A
authors.lastname: Mehta
authors.forename: Lynn
authors.initials: L
authors.lastname: Rasmussen
authors.forename: Robert C
authors.initials: RC
authors.lastname: Reynolds
authors.forename: John A
authors.initials: JA
authors.lastname: Secrist
authors.forename: Nice
authors.initials: N
authors.lastname: Shindo
authors.forename: Dustin N
authors.initials: DN
authors.lastname: Showe
authors.forename: Melinda I
authors.initials: MI
authors.lastname: Sosa
authors.forename: William J
authors.initials: WJ
authors.lastname: Suling
authors.forename: E Lucile
authors.initials: EL
authors.lastname: White
mesh_terms: 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
chemical_list: D000995:Antitubercular Agents; D001426:Bacterial Proteins; D007155:Immunologic Factors; D054852:Small Molecule Libraries