In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
The diarylquinoline R207910 is in clinical development for tuberculosis treatment. The MIC(50) for 41 drug-susceptible and 44 multidrug-resistant Mycobacterium tuberculosis clinical isolates was 0.032 microg/ml. Out of 20 additional mycobacterial species, three were found to be naturally resistant to R207910 and were shown to exhibit a polymorphism in their atpE genes.
Huitric
Emma
E
Department of Bacteriology, Swedish Institute for Infectious Disease Control, S-171 82 Solna, Sweden. emma.huitric@smi.ki.se
Verhasselt
Peter
P
Andries
Koen
K
Hoffner
Sven E
SE
D025181:ATP Synthetase Complexes / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D000595:Amino Acid Sequence; D000995:Antitubercular Agents / Q000494:pharmacology*; D064687:Diarylquinolines; D024881:Drug Resistance, Bacterial; D008826:Microbial Sensitivity Tests; D008969:Molecular Sequence Data; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000201:enzymology / Q000235:genetics; D011110:Polymorphism, Genetic; D011804:Quinolines / Q000494:pharmacology*; D017386:Sequence Homology, Amino Acid
D000995:Antitubercular Agents; D064687:Diarylquinolines; D011804:Quinolines; C493870:bedaquiline; D025181:ATP Synthetase Complexes
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