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Publication: In vitro efficacies, ADME, and pharmacokinetic properties of phenoxazine derivatives active against Mycobacterium tuberculosis
Tanner, L Evans, J.C Seldon, R Seldon, A Warner, D.F Haynes, R.K Parkinson, C.J Wiesner, L
Tanner, L
Evans, J.C
Seldon, R
Seldon, A
Warner, D.F
Haynes, R.K
Parkinson, C.J
Wiesner, L
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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.
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Date
2019-08-19
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Publisher
American Society for Microbiology
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Research Projects
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Keywords
ADME,TB chemotherapy,Pharmacokinetics,Phenoxazines
Citation
Tanner L, Evans JC, Seldon R, Jordaan A, Warner DF, Haynes RK, Parkinson CJ, Wiesner L. In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2019 Oct 22;63(11):e01010-19. doi: 10.1128/AAC.01010-19.