Diarylquinoline - Wikipedia
Diaryl quinolines (DARQs) are a chemical class of drugs that treat tuberculosis. They target subunit c of mycobacterial ATP ... Although ATP synthase in bacteria is similar to its eukaryotic analogue, diarylquinoline agents (such as TMC207) are very ... Metal free synthesis of 2,4-diarylquinoline derivatives with enamides and imines (Articles with short description, Short ... 4-diaryl quinoline (phenyl and naphthyl). US FDA approval in 2012. As of 2014, the only licensed indication of the drug ...
Provisional CDC Guidelines for the Use and Safety Monitoring of Bedaquiline Fumarate (Sirturo) for the Treatment of Multidrug...
Bedaquiline fumarate (Sirturo or bedaquiline) is an oral diarylquinoline. On December 28, 2012, on the basis of data from two ... Bedaquiline, a diarylquinoline, is the first drug with a novel mechanism of action against M. tuberculosis that has been ... The diarylquinoline TMC207 for multidrug-resistant tuberculosis. N Engl J Med 2009;360:2397-405 10.1056/NEJMoa0808427. ...
Rates and mechanisms of resistance development in **Mycobacterium tuberculosis** to a novel diarylquinoline ATP synthase...
Copper(ii) triflate catalyzed three-component reaction for the synthesis of 2,3-diarylquinoline derivatives using aryl amines,...
Ali, S., & Khan, A. T. (2021). Copper(ii) triflate catalyzed three-component reaction for the synthesis of 2,3-diarylquinoline ... Ali, Saghir ; Khan, Abu T. / Copper(ii) triflate catalyzed three-component reaction for the synthesis of 2,3-diarylquinoline ... Ali, S & Khan, AT 2021, Copper(ii) triflate catalyzed three-component reaction for the synthesis of 2,3-diarylquinoline ... Copper(ii) triflate catalyzed three-component reaction for the synthesis of 2,3-diarylquinoline derivatives using aryl amines, ...
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A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science. 2005;307(5707):223-227.. View this ... Diarylquinolines are bactericidal for dormant mycobacteria as a result of disturbed ATP homeostasis. J Biol Chem. 2008;283(37): ... Genetic basis for natural and acquired resistance to the diarylquinoline R207910 in mycobacteria. Antimicrob Agents Chemother. ...
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Sirturo (bedaquiline) dosing, indications, interactions, adverse effects, and more
Diarylquinoline; inhibits mycobacterial adenosine 5-triphosphate (ATP) synthase, an enzyme essential for the generation of ... Diarylquinoline antimycobacterial indicated as part of combination therapy for pulmonary multidrug resistant tuberculosis (MDR- ... Diarylquinoline antimycobacterial indicated as part of combination therapy for pulmonary multidrug resistant tuberculosis (MDR- ...
U.S. FDA Grants Priority Review to Bedaquiline (TMC207) for Multi-Drug Resistant Tuberculosis Treatment | Johnson & Johnson
Frontiers | In vitro Study of Bedaquiline Resistance in Mycobacterium tuberculosis Multi-Drug Resistant Clinical Isolates
BDQ is a diarylquinoline that targets atpE gene, coding for the subunit c of the ATP synthase complex (Andries et al., 2005). ... 2005). A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 307, 223-227. doi: 10.1126/ ... new insights into the binding of the diarylquinoline TMC207 to the ATP synthase C-ring structure. Antimicrob. Agents Chemother. ... Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor ...
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The diarylquinoline bedaquiline (BDQ), a mycobacterial ATP synthase inhibitor, is used for treatment of drug-resistant ... 2023). Mechanism of mycobacterial ATP synthase inhibition by squaramides and second generation diarylquinolines. EMBO. J. ... which may explain why high concentrations of diarylquinolines, but not SQ31f, have been reported to kill mycobacteria (Courbon ... and high concentrations of the diarylquinolines uncouple the transmembrane proton motive force while for SQ31f they do not, ...
Sirturo (bedaquiline) dosing, indications, interactions, adverse effects, and more
Diarylquinoline; inhibits mycobacterial adenosine 5-triphosphate (ATP) synthase, an enzyme essential for the generation of ... Diarylquinoline antimycobacterial indicated as part of combination therapy for pulmonary multidrug resistant tuberculosis (MDR- ... Diarylquinoline antimycobacterial indicated as part of combination therapy for pulmonary multidrug resistant tuberculosis (MDR- ...
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Probing the interaction of the diarylquinoline TMC207 with its target mycobacterial ATP synthase. PLoS One, 2011, 6(8), e23575. ... Diarylquinolines target subunit c of mycobacterial ATP synthase. Nat. Chem. Biol., 2007, 3(6), 323-324.. [http://dx.doi.org/ ... A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science, 2005, 307(5707), 223-227.. [http://dx ...
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Bedaquiline - WikiProjectMed
June 2009). "The diarylquinoline TMC207 for multidrug-resistant tuberculosis". The New England Journal of Medicine. 360 (23): ... It is in the diarylquinoline antimycobacterial class of medications.[1] It works by blocking the ability of M. tuberculosis to ... It is the first member of a new class of drugs called the diarylquinolines.[19] Bedaquiline is bactericidal.[19] ATP production ...
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Gelber R, Andries K, Paredes RM, Andaya CE, Burgos J. The diarylquinoline R207910 is bactericidal against Mycobacterium leprae ... In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor. Antimicrob Agents Chemother. 2007;51:4202-4. ... Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. ...
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