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Stewart Cole

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Page 6 of 49

New 1-hydroxy-2-thiopyridine derivatives active against both replicating and dormant Mycobacterium tuberculosis

Stewart Cole, Anthony Vocat

Tuberculosis (TB) treatment is confounded by the range of metabolic states displayed by Mycobacterium tuberculosis, by the long duration required and by the increasing prevalence of drug-resistant strains. Latent TB infection is especially difficult to tre ...

Elsevier Science Bv2017

Insights from the Genome Sequence of Mycobacterium lepraemurium: Massive Gene Decay and Reductive Evolution

Stewart Cole, Andrej Benjak, Charlotte Avanzi

Mycobacterium lepraemurium is the causative agent of murine leprosy, a chronic, granulomatous disease similar to human leprosy. Due to the similar clinical manifestations of human and murine leprosy and the difficulty of growing both bacilli axenically, My ...

Amer Soc Microbiology2017

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria

Stewart Cole, Kai Johnsson, John McKinney, Graham Knott, Neeraj Dhar, Ruben Hartkoorn, Anthony Vocat, Gaëlle Séraphine Kolly, Jan Lars Rybniker, Edina Rita Székely, François Signorino-Gelo, Isabella Santi, Monica Rengifo Gonzalez

There is an urgent need to discover new antitubercular agents with novel mechanisms of action in order to tackle the scourge of drug-resistant tuberculosis. Here, we report the identification of such a molecule - an AminoPYrimidine-Sulfonamide (APYS1) that ...

Wiley-Blackwell2017

Synthesis of Adamantane Aminoethers with Antitubercular Potential

Stewart Cole, Anthony Vocat

Background: Intrigued by the fact that aminoadamantane derivatives, bearing the active 1,2-ethylenediamine moiety, are promising antitubercular agents, we report herein the synthesis and the antitubercular evaluation of N,N'-substituded-4,4'-[adamantane-2, ...

Bentham Science Publ Ltd2017

Transcription facilitated genome-wide recruitment of topoisomerase I and DNA gyrase

Stewart Cole, Claudia Sala, Wareed Ahmed

Movement of the transcription machinery along a template alters DNA topology resulting in the accumulation of supercoils in DNA. The positive supercoils generated ahead of transcribing RNA polymerase (RNAP) and the negative supercoils accumulating behind i ...

Public Library Science2017

NOS2-deficient mice with hypoxic necrotizing lung lesions predict outcomes of tuberculosis chemotherapy in humans

Stewart Cole

During active TB in humans a spectrum of pulmonary granulomas with central necrosis and hypoxia exists. BALB/c mice, predominantly used in TB drug development, do not reproduce this complex pathology thereby inaccurately predicting clinical outcome. We fou ...

Nature Publishing Group2017

Tuberculosis drug discovery needs public-private consortia

Stewart Cole

Elsevier Sci Ltd2017

In vitro Controlled Release from Solid Pharmaceutical Formulations of two new Adamantane Aminoethers with Antitubercular Activity (I).

Stewart Cole, Anthony Vocat

The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of 2 new tuberculocidal adamantane aminoethers (compounds I and II), congeneric to the adamantane derivative SQ109 , which is in final clinic ...

Georg Thieme Verlag Kg2017

Genomic and transcriptomic analysis of the streptomycin-dependent Mycobacterium tuberculosis strain 18b

Stewart Cole, Claudia Sala, Andrej Benjak, Ming Zhang, Jérémie Piton, Swapna Uplekar

Background: The ability of Mycobacterium tuberculosis to establish a latent infection (LTBI) in humans confounds the treatment of tuberculosis. Consequently, there is a need to discover new therapeutic agents that can kill M. tuberculosis both during activ ...

BioMed Central2016

Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis

Stewart Cole, Stefanie Boy-Röttger, Claudia Sala, Jérémie Piton, Gaëlle Séraphine Kolly, Joao Pedro De Almeida Neres, Jan Lars Rybniker, Benoit Lechartier, Shi-Yan Caroline Foo, Andréanne Lupien

Benzothiazinones (BTZs) are a class of compounds found to be extremely potent against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. The potency of BTZs is explained by their specificity for their target decaprenylphosphoryl-D ...

American Society for Microbiology2016

Synthesis of Adamantane Aminoethers with Antitubercular Potential

Stewart Cole, Anthony Vocat

Bentham Science Publ Ltd2017

Tuberculosis drug discovery needs public-private consortia

Stewart Cole

Elsevier Sci Ltd2017

In vitro Controlled Release from Solid Pharmaceutical Formulations of two new Adamantane Aminoethers with Antitubercular Activity (I).

Stewart Cole, Anthony Vocat

Georg Thieme Verlag Kg2017