A tale of two inhibitors: diarylquinolines and squaramides. [PDF]
EMBO J, 2023 The diarylquinoline bedaquiline (BDQ) is an FDA‐approved drug for the treatment of multidrug‐resistant tuberculosis that targets the mycobacterial adenosine triphosphate (ATP) synthase, a key enzyme in cellular respiration. In a recent study, Courbon et al (2023) examine the interaction ...
Chen J, Ekiert DC.
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Mechanism of mycobacterial ATP synthase inhibition by squaramides and second generation diarylquinolines. [PDF]
EMBO J, 2023 Abstract Mycobacteria, such as Mycobacterium tuberculosis , depend on the activity of adenosine triphosphate (ATP) synthase for growth. The diarylquinoline bedaquiline (BDQ), a mycobacterial ATP synthase inhibitor, is an important medication for treatment of drug‐resistant ...
Courbon GM +5 more
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Fabrication of Fe3O4@UiO-66-NH2-QCA-CuCl2 nanocomposites as a novel magnetic metal–organic framework catalyst for sustainable synthesis of 2,3-diarylquinolines [PDF]
BMC ChemistryIn this study, a novel magnetic metal–organic framework catalyst, Fe3O4@UiO-66-NH2-QCA-CuCl2, was successfully fabricated and thoroughly characterized to confirm its structural and functional properties.
Zahra Moghadasi +7 more
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Therapeutic Failure and Acquired Bedaquiline and Delamanid Resistance in Treatment of Drug-Resistant TB [PDF]
Emerging Infectious Diseases, 2023 New classes of antitubercular drugs, diarylquinolines and nitroimidazoles, have been associated with improved outcomes in the treatment of drug-resistant tuberculosis, but that success is threatened by emerging drug resistance.
James Millard +3 more
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Discovery of a Novel Mycobacterial F‐ATP Synthase Inhibitor and its Potency in Combination with Diarylquinolines [PDF]
Angewandte Chemie - International Edition, 2020 AbstractThe F1FO‐ATP synthase is required for growth and viability of Mycobacterium tuberculosis and is a validated clinical target. A mycobacterium‐specific loop of the enzyme's rotary γ subunit plays a role in the coupling of ATP synthesis within the enzyme complex. We report the discovery of a novel antimycobacterial, termed GaMF1, that targets this
Adam Hotra +2 more
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Diarylquinolines Are Bactericidal for Dormant Mycobacteria as a Result of Disturbed ATP Homeostasis [PDF]
Journal of Biological Chemistry, 2008 An estimated one-third of the world population is latently infected with Mycobacterium tuberculosis. These nonreplicating, dormant bacilli are tolerant to conventional anti-tuberculosis drugs, such as isoniazid. We recently identified diarylquinoline R207910 (also called TMC207) as an inhibitor of ATP synthase with a remarkable activity against ...
Anil Koul +2 more
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2,4-Diarylquinolines: Synthesis, Absorption and Emission Properties
Journal of Chemical Research, 2014 The absorption and emission spectra of series of 2,4-diarylquinolines prepared via palladium catalysed Suzuki-Miyaura cross-coupling of 2-aryl-4-chloroquinolines with arylboronic acids were measured in solution to understand the influence of substituents on intramolecular charge transfer.
Adewale O Adeloye, Malose J Mphahlele
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Potential targets for the new anti-tuberculosis drug of the diarylquinoline group thiozonide
Разработка и регистрация лекарственных средствIntroduction. Diarylquinolines are considered a group of optimal candidates for anti-tuberculosis drugs (ATDs) in the treatment of tuberculosis caused by Mycobacterium tuberculosis exhibiting multidrug resistance.Aim. To perform a computer-aided analysis
А. Yu. Savchenko, B. V. Shilov
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Bi(OTf)3-Catalyzed Cascade Cycloaddition-Decarbonylation-N-Deoxygenative Aromatization between 2-Arylisatogens and Styrenes: Unveiling a Synthesis of 2,4-Diarylquinolines. [PDF]
Org LettAn unprecedented Bi(OTf)3-catalyzed reaction between 2-arylisatogens and vinylarenes to yield 2,4-diarylquinolines is reported. The transformation occurred via a BiIII-coordination to the embedded anionic nitrone oxygen, which induced a regiospecific ...
Punjajom K +4 more
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Next-Generation Diarylquinolines Improve Sterilizing Activity of Regimens with Pretomanid and the Novel Oxazolidinone TBI-223 in a Mouse Tuberculosis Model. [PDF]
Antimicrob Agents Chemother, 2023 A regimen comprised of bedaquiline (BDQ, or B), pretomanid, and linezolid (BPaL) is the first oral 6-month regimen approved by the U.S. Food and Drug Administration and recommended by the World Health Organization for the treatment of extensively drug ...
Li SY +7 more
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