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A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis

A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis

http://www.wikidata.org/entity/Q27004482

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TB drug development: immunology at the table Looking back to the future: predicting in vivo efficacy of small molecules versus Mycobacterium tuberculosis Cytokine Kinetics in the First Week of Tuberculosis Therapy as a Tool to Confirm a Clinical Diagnosis and Guide Therapy In silico evaluation and exploration of antibiotic tuberculosis treatment regimens Are bigger data sets better for machine learning? Fusing single-point and dual-event dose response data for Mycobacterium tuberculosis Predicting Mouse Liver Microsomal Stability with "Pruned" Machine Learning Models and Public Data.The efflux pump inhibitor timcodar improves the potency of antimycobacterial agents.Anti-vascular endothelial growth factor treatment normalizes tuberculosis granuloma vasculature and improves small molecule delivery.The path of anti-tuberculosis drugs: from blood to lesions to mycobacterial cells.Mycobacterium tuberculosis metabolism Fragment-based exploration of binding site flexibility in Mycobacterium tuberculosis BioA.The tuberculosis drug discovery and development pipeline and emerging drug targets.Presence of multiple lesion types with vastly different microenvironments in C3HeB/FeJ mice following aerosol infection with Mycobacterium tuberculosis.Genetic Approaches to Facilitate Antibacterial Drug Development.Design and Synthesis of a Focused Library of Diamino Triazines as Potential Mycobacterium tuberculosis DHFR Inhibitors Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes In vitro and in vivo Evaluation of Synergism between Anti-Tubercular Spectinamides and Non-Classical Tuberculosis Antibiotics Fragment-Based Whole Cell Screen Delivers Hits against M. tuberculosis and Non-tuberculous Mycobacteria.Using Chemical Reaction Kinetics to Predict Optimal Antibiotic Treatment Strategies.Reaction intermediate analogues as bisubstrate inhibitors of pantothenate synthetase.Stereocontrolled Synthesis of a Potential Transition-State Inhibitor of the Salicylate Synthase MbtI from Mycobacterium tuberculosis.Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.Synthesis and pharmacological evaluation of nucleoside prodrugs designed to target siderophore biosynthesis in Mycobacterium tuberculosis.Quantifying Limits on Replication, Death, and Quiescence of Mycobacterium tuberculosis in Mice.Bioluminescent Reporters for Rapid Mechanism of Action Assessment in Tuberculosis Drug Discovery.A Bioengineered Three-Dimensional Cell Culture Platform Integrated with Microfluidics To Address Antimicrobial Resistance in Tuberculosis.Spectinamides: a new class of semisynthetic antituberculosis agents that overcome native drug efflux A temporal proteome dynamics study reveals the molecular basis of induced phenotypic resistance in Mycobacterium smegmatis at sub-lethal rifampicin concentrations Targeting dormant bacilli to fight tuberculosis.Tuberculosis drug discovery and emerging targets.Nucleoside analogs and tuberculosis: new weapons against an old enemy.The anti-tuberculosis agents under development and the challenges ahead.Comprehensive physicochemical, pharmacokinetic and activity profiling of anti-TB agents.Targeting Phenotypically Tolerant Mycobacterium tuberculosis.Targeting DNA Replication and Repair for the Development of Novel Therapeutics against Tuberculosis.Evolution of Phenotypic and Molecular Drug Susceptibility Testing.Novel Pyrimidines as Antitubercular Agents.Design, Synthesis, and Biological Evaluation of 1,4-dihydropyridine Derivatives as Potent Antitubercular Agents.Is IQG-607 a Potential Metallodrug or Metallopro-Drug With a Defined Molecular Target in Mycobacterium tuberculosis?The importance of clinical pharmacokinetic-pharmacodynamic studies in unraveling the determinants of early and late tuberculosis outcomes

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A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis

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Multiple M. tuberculosis phenotypes in mouse and guinea pig lung tissue revealed by a dual-staining approach

Daily dosing of rifapentine cures tuberculosis in three months or less in the murine model

Global and regional mortality from 235 causes of death for 20 age groups in 1990 and 2010: a systematic analysis for the Global Burden of Disease Study 2010

Fluoroquinolones for treating tuberculosis

Studies on the treatment of tuberculosis undertaken by the British Medical Research Council tuberculosis units, 1946-1986, with relevant subsequent publications

An in vitro model for sequential study of shiftdown of Mycobacterium tuberculosis through two stages of nonreplicating persistence

Fluoroquinolone action in mycobacteria: similarity with effects in Escherichia coli and detection by cell lysate viscosity

Phosphodiesterase-4 inhibition combined with isoniazid treatment of rabbits with pulmonary tuberculosis reduces macrophage activation and lung pathology

Serine protease activity contributes to control of Mycobacterium tuberculosis in hypoxic lung granulomas in mice

Ipr1 gene mediates innate immunity to tuberculosis.

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