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In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis.


ABSTRACT: Mycobacterium tuberculosis, the causative agent of tuberculosis, remains a leading infectious killer globally, demanding the urgent development of faster-acting drugs with novel mechanisms of action. Riminophenazines such as clofazimine are clinically efficacious against both drug-susceptible and drug-resistant strains of M. tuberculosis We determined the in vitro anti-M. tuberculosis activities, absorption, distribution, metabolism, and excretion properties, and in vivo mouse pharmacokinetics of a series of structurally related phenoxazines. One of these, PhX1, displayed promising drug-like properties and potent in vitro efficacy, supporting its further investigation in an M. tuberculosis-infected animal model.

SUBMITTER: Tanner L 

PROVIDER: S-EPMC6811447 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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<i>In Vitro</i> Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis.

Tanner Lloyd L   Evans Joanna C JC   Seldon Ronnett R   Jordaan Audrey A   Warner Digby F DF   Haynes Richard K RK   Parkinson Christopher J CJ   Wiesner Lubbe L  

Antimicrobial agents and chemotherapy 20191022 11


<i>Mycobacterium tuberculosis</i>, the causative agent of tuberculosis, remains a leading infectious killer globally, demanding the urgent development of faster-acting drugs with novel mechanisms of action. Riminophenazines such as clofazimine are clinically efficacious against both drug-susceptible and drug-resistant strains of <i>M. tuberculosis</i> We determined the <i>in vitro</i> anti-<i>M. tuberculosis</i> activities, absorption, distribution, metabolism, and excretion properties, and <i>i  ...[more]

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