In Vitro efficacies, ADME, and Pharmacokinetic properties of Phenoxazine Derivatives active against Mycobacterium tuberculosis

Lloyd Tanner, Joanna C. Evans, Ronnett Seldon, Audrey Jordaan, Digby F. Warner, Richard K. Haynes, Christopher J. Parkinson, Lubbe Wiesner

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

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.
Original languageEnglish
Article numbere01010-19
Pages (from-to)1-10
Number of pages10
JournalAntimicrobial Agents and Chemotherapy
Volume63
Issue number11
Early online date22 Oct 2019
DOIs
Publication statusPublished - 01 Nov 2019

Fingerprint

Dive into the research topics of '<i>In Vitro</i> efficacies, ADME, and Pharmacokinetic properties of Phenoxazine Derivatives active against <i>Mycobacterium tuberculosis</i>'. Together they form a unique fingerprint.

Cite this