An in vitro ADME and in vivo Pharmacokinetic Study of Novel TB-Active Decoquinate Derivatives.

ABSTRACT: Tuberculosis (TB) is currently the leading cause of mortality due to an infectious disease, despite the existence of multiple effective first-line and second-line drugs. The current anti-TB regimen requires a prolonged treatment period of around 6 months and is only efficacious against drug-sensitive strains of Mycobacterium tuberculosis (Mtb). With a rise in cases of multi-drug resistant and extensively drug resistant strains of Mtb, newer treatments comprising compounds with novel mechanisms of action are required. Although decoquinate (DQ) is inactive against Mtb, its derivatives are of interest to anti-TB drug discovery because of their potential to permeate the mycobacterial cell wall, Mtb-infected macrophages, and granulomatous lesions by passive diffusion. The compounds also display

SUBMITTER: Tanner L 

PROVIDER: S-EPMC6387968 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature