Discovery and development of SQ109: a new antitubercular drug with a novel mechanism of action

KA Sacksteder, M Protopopova, CE Barry… - Future …, 2012 - Future Medicine
Existing drugs have limited efficacy against the rising threat of drug-resistant TB, have
significant side effects, and must be given in combinations of four to six drugs for at least 6 …

Tuberculosis drug discovery in the post‐post‐genomic era

B Lechartier, J Rybniker, A Zumla… - EMBO molecular …, 2014 - embopress.org
The expectation that genomics would result in new therapeutic interventions for infectious
diseases remains unfulfilled. In the post‐genomic era, the decade immediately following the …

Novel insights into the mechanism of inhibition of MmpL3, a target of multiple pharmacophores in Mycobacterium tuberculosis

W Li, A Upadhyay, FL Fontes, EJ North… - Antimicrobial agents …, 2014 - Am Soc Microbiol
ABSTRACT MmpL3, a resistance-nodulation-division (RND) superfamily transporter, has
been implicated in the formation of the outer membrane of Mycobacterium tuberculosis; …

[HTML][HTML] Mycobacterium tuberculosis and whole-genome sequencing: how close are we to unleashing its full potential?

G Satta, M Lipman, GP Smith, C Arnold, OM Kon… - Clinical Microbiology …, 2018 - Elsevier
Background Nearly two decades after completion of the genome sequence of
Mycobacterium tuberculosis (MTB), and with the advent of next generation sequencing …

Therapeutic potential of the Mycobacterium tuberculosis mycolic acid transporter, MmpL3

W Li, A Obregón-Henao, JB Wallach… - Antimicrobial agents …, 2016 - Am Soc Microbiol
In recent years, whole-cell-based screens for novel small molecule inhibitors active against
Mycobacterium tuberculosis in culture followed by the whole-genome sequencing of …

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

J Neres, RC Hartkoorn, LR Chiarelli… - ACS chemical …, 2015 - ACS Publications
Phenotypic screening of a quinoxaline library against replicating Mycobacterium
tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl) amino) …

In Vitro Combination Studies of Benzothiazinone Lead Compound BTZ043 against Mycobacterium tuberculosis

B Lechartier, RC Hartkoorn, ST Cole - Antimicrobial agents and …, 2012 - Am Soc Microbiol
Benzothiazinones (BTZ) are a new class of drug candidates to combat tuberculosis that
inhibit decaprenyl-phosphoribose epimerase (DprE1), an essential enzyme involved in …

Synthetic account of indoles in search of potential anti-mycobacterial agents: a review and future insights

KA Bhakhar, DK Sureja, TM Dhameliya - Journal of Molecular Structure, 2022 - Elsevier
Indole, an aza-heterocyclic scaffold, has been found one of the most privileged scaffolds in
heterocyclic chemistry and drug discovery. Efforts have been made to provide the complete …

Progress in targeting cell envelope biogenesis in Mycobacterium tuberculosis

M Jackson, MR McNeil, PJ Brennan - Future microbiology, 2013 - Future Medicine
Most of the newly discovered compounds showing promise for the treatment of TB, notably
multidrug-resistant TB, inhibit aspects of Mycobacterium tuberculosis cell envelope …

Liposomes as drug delivery systems for the treatment of TB

M Pinheiro, M Lúcio, JLFC Lima, S Reis - Nanomedicine, 2011 - Future Medicine
TB is an infectious disease that is far from being eradicated and controlled. The treatment for
TB is associated with noncompliance to therapy because it consists of a long-term treatment …