Development of potent chemical antituberculosis agents targeting Mycobacterium tuberculosis acetohydroxyacid synthase

Highlights • 15 chemical inhibitors against Mycobacterium tuberculosis acetohydroxyacid synthase (MTB-AHAS) were identified. • Five hit compounds showed high inhibition against MTB-AHAS at low micromolar concentrations. • Five hit compounds exhibited anti-mycobacterial activity against drug-resistan...

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Veröffentlicht in:	International journal of antimicrobial agents 2016-09, Vol.48 (3), p.247-258
Hauptverfasser:	Jung, In-Pil, Ha, Na-Reum, Lee, Sang-Choon, Ryoo, Sung-Weon, Yoon, Moon-Young
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetohydroxyacid synthase Acetolactate Synthase - antagonists & inhibitors Acetolactate Synthase - chemistry Antitubercular Agents - chemistry Antitubercular Agents - isolation & purification Antitubercular Agents - pharmacology Cytotoxicity Drug Evaluation, Preclinical Drug-resistant TB Enzyme Inhibitors - chemistry Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - pharmacology High-Throughput Screening Assays Humans Infectious Disease Inhibitory Concentration 50 Microbial Sensitivity Tests Molecular docking Molecular Docking Simulation Mycobacterium tuberculosis Mycobacterium tuberculosis - drug effects Mycobacterium tuberculosis - enzymology Mycobacterium tuberculosis - isolation & purification Potent inhibitor Protein Binding Tuberculosis, Multidrug-Resistant - microbiology
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Zusammenfassung:	Highlights • 15 chemical inhibitors against Mycobacterium tuberculosis acetohydroxyacid synthase (MTB-AHAS) were identified. • Five hit compounds showed high inhibition against MTB-AHAS at low micromolar concentrations. • Five hit compounds exhibited anti-mycobacterial activity against drug-resistant M. tuberculosis strains with MICs of 0.5–2 μM. • Two inhibitors among the hit compounds specifically inhibited Escherichia coli expressing MTB-AHAS.
ISSN:	0924-8579 1872-7913
DOI:	10.1016/j.ijantimicag.2016.04.031