Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
A novel subclass of quinolones, 2-pyridones, showed potent activity against Mycobacterium tuberculosis, with KRQ-10018 being an early lead. KRQ-10018 showed better activity in vitro against M. tuberculosis versus moxifloxacin. In vivo efficacy of KRQ-10018 at 300 mg/kg of body weight was similar to that of isoniazid at 25 mg/kg, but showed less activity than moxifloxacin at 300 mg/kg.
Lenaerts
Anne J
AJ
Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, CO 80523, USA. lenaerts@colostate.edu
Bitting
Casey
C
Woolhiser
Lisa
L
Gruppo
Veronica
V
Marietta
Karen S
KS
Johnson
Christine M
CM
Orme
Ian M
IM
D000818:Animals; D000995:Antitubercular Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use*; D001682:Biological Availability; D007371:Interferon-gamma / Q000235:genetics; D051379:Mice; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011728:Pyridones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use*; D015363:Quinolones / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D016896:Treatment Outcome; D014397:Tuberculosis, Pulmonary / Q000188:drug therapy* / Q000382:microbiology
D000995:Antitubercular Agents; D011728:Pyridones; D015363:Quinolones; C017679:2-hydroxypyridine; D007371:Interferon-gamma