In vitro efficacies, ADME, and pharmacokinetic properties of phenoxazine derivatives active against Mycobacterium tuberculosis.

In vitro efficacies, ADME, and pharmacokinetic properties of phenoxazine derivatives active against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2019 Aug 19;: Authors: Tanner L, Evans JC, Seldon R, Jordaan A, Warner DF, Haynes RK, Parkinson CJ, Wiesner L Abstract Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), 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 Mtb. We determined the in vitro anti-Mtb 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 Mtb-infected animal model. PMID: 31427302 [PubMed - as supplied by publisher]
Source: Antimicrobial Agents and Chemotherapy - Category: Microbiology Authors: Tags: Antimicrob Agents Chemother Source Type: research