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Identify and evaluate the antimycobacterial potency, therapeutic potential, and mechanism of action of the diarylquinoline R207910 against Mycobacterium tuberculosis.

December 9, 2004ScienceOpen Access

A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis

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Identify and evaluate the antimycobacterial potency, therapeutic potential, and mechanism of action of the diarylquinoline R207910 against Mycobacterium tuberculosis.
Screened R207910 in vitro against drug-sensitive and drug-resistant Mycobacterium tuberculosis strains and sequenced resistant mutants to identify the molecular target.
Assessed bactericidal efficacy, dosing schedules, and first-line substitution regimens in murine tuberculosis models, and evaluated drug tolerability in healthy human volunteers.
R207910 potently inhibited drug-sensitive and drug-resistant M. tuberculosis in vitro with a minimum inhibitory concentration of 0.06 µg/ml.
In mice, R207910 surpassed the bactericidal activity of isoniazid and rifampin by at least 1 log unit and achieved complete culture conversion at 2 months in combination regimens.
Target analysis demonstrated inhibition of the proton pump of mycobacterial ATP synthase, with effective murine plasma concentrations proving well tolerated in humans.

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Implication

Preclinical evaluation reveals potent bactericidal activity of diarylquinoline R207910 against Mycobacterium tuberculosis, indicating potential to shorten treatment regimens.

Cite This Study

Andries et al. (2004) studied this question.

synapsesocial.com/papers/69d7504bf182769aa8b8a3ba https://doi.org/10.1126/science.1106753

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Implication

Preclinical evaluation reveals potent bactericidal activity of diarylquinoline R207910 against Mycobacterium tuberculosis, indicating potential to shorten treatment regimens.

A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis

Key Points

Discussion

Implication

Cite This Study

A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis

Key Points

Discussion

Implication

Cite This Study

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