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Agents Chemother."},{"key":"10.1016\/j.ejmech.2018.03.020_bib69","doi-asserted-by":"crossref","first-page":"5585","DOI":"10.1016\/j.bmc.2011.07.034","article-title":"The structure-activity relationship of urea derivatives as anti-tuberculosis agents","volume":"19","author":"Brown","year":"2011","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2018.03.020_bib70","doi-asserted-by":"crossref","first-page":"3255","DOI":"10.1016\/j.bmc.2012.03.058","article-title":"Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in\u00a0vitro and for better physical chemical properties for bioavailability","volume":"20","author":"Scherman","year":"2012","journal-title":"Bioorg. Med. 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Rep."},{"key":"10.1016\/j.ejmech.2018.03.020_bib137","doi-asserted-by":"crossref","first-page":"572","DOI":"10.1107\/S1744309106016824","article-title":"Overexpression, purification and crystallization of lysine epsilon-aminotransferase (Rv3290c) from Mycobacterium tuberculosis H37Rv","volume":"62","author":"Tripathi","year":"2006","journal-title":"Acta Crystallogr F Struct Biol"},{"key":"10.1016\/j.ejmech.2018.03.020_bib138","doi-asserted-by":"crossref","first-page":"786","DOI":"10.1016\/j.tube.2015.04.010","article-title":"Discovery of novel lysine varepsilon-aminotransferase inhibitors: an intriguing potential target for latent tuberculosis","volume":"95","author":"Devi","year":"2015","journal-title":"Tuberculosis"},{"key":"10.1016\/j.ejmech.2018.03.020_bib139","doi-asserted-by":"crossref","first-page":"2761","DOI":"10.1016\/j.bmc.2017.03.053","article-title":"Mycobacterium tuberculosis lysine-varepsilon-aminotransferase a potential target in dormancy: benzothiazole based inhibitors","volume":"25","author":"Reshma","year":"2017","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2018.03.020_bib140","first-page":"79","article-title":"Compound management for quantitative high-throughput screening","volume":"13","author":"Yasgar","year":"2008","journal-title":"JALA"},{"key":"10.1016\/j.ejmech.2018.03.020_bib141","doi-asserted-by":"crossref","first-page":"11473","DOI":"10.1073\/pnas.0604348103","article-title":"Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries","volume":"103","author":"Inglese","year":"2006","journal-title":"Proc. Natl. Acad. Sci. U.S.A."},{"key":"10.1016\/j.ejmech.2018.03.020_bib142","doi-asserted-by":"crossref","first-page":"658","DOI":"10.1107\/S0021889807021206","article-title":"Phaser crystallographic software","volume":"40","author":"McCoy","year":"2007","journal-title":"J.\u00a0Appl. Crystallogr."},{"key":"10.1016\/j.ejmech.2018.03.020_bib143","doi-asserted-by":"crossref","first-page":"355","DOI":"10.1107\/S0907444911001314","article-title":"REFMAC5 for the refinement of macromolecular crystal structures","volume":"67","author":"Murshudov","year":"2011","journal-title":"Acta crystallogr D Biol Cryst"},{"key":"10.1016\/j.ejmech.2018.03.020_bib144","doi-asserted-by":"crossref","first-page":"235","DOI":"10.1107\/S0907444910045749","article-title":"Overview of the CCP4 suite and current developments","volume":"67","author":"Winn","year":"2011","journal-title":"Acta crystallogr D Biol Cryst"},{"key":"10.1016\/j.ejmech.2018.03.020_bib145","doi-asserted-by":"crossref","first-page":"7503","DOI":"10.1073\/pnas.1600630113","article-title":"Selective small molecule inhibitor of the Mycobacterium tuberculosis fumarate hydratase reveals an allosteric regulatory site","volume":"113","author":"Kasbekar","year":"2016","journal-title":"Proc. Natl. Acad. Sci. U.S.A."},{"key":"10.1016\/j.ejmech.2018.03.020_bib146","doi-asserted-by":"crossref","first-page":"457","DOI":"10.1038\/nrd.2017.23","article-title":"Different drugs for bad bugs: antivirulence strategies in the age of antibiotic resistance","volume":"16","author":"Dickey","year":"2017","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2018.03.020_bib147","doi-asserted-by":"crossref","first-page":"569","DOI":"10.1016\/j.tube.2013.09.003","article-title":"Why are membrane targets discovered by phenotypic screens and genome sequencing in Mycobacterium tuberculosis?","volume":"93","author":"Goldman","year":"2013","journal-title":"Tuberculosis"},{"key":"10.1016\/j.ejmech.2018.03.020_bib148","doi-asserted-by":"crossref","first-page":"357","DOI":"10.1016\/j.tube.2014.04.001","article-title":"Bedaquiline for the treatment of resistant tuberculosis: promises and pitfalls","volume":"94","author":"Kakkar","year":"2014","journal-title":"Tuberculosis"},{"key":"10.1016\/j.ejmech.2018.03.020_bib149","unstructured":"WHO - World Health Organization, in www.who.int, accessed March 3, 2018."},{"key":"10.1016\/j.ejmech.2018.03.020_bib150","unstructured":"TB Alliance, in https:\/\/www.tballiance.org\/, accessed March 3, 2018."},{"key":"10.1016\/j.ejmech.2018.03.020_bib151","doi-asserted-by":"crossref","first-page":"821","DOI":"10.1038\/nrd4675","article-title":"Antibiotic resistance breakers: can repurposed drugs fill the antibiotic discovery void?","volume":"14","author":"Brown","year":"2015","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2018.03.020_bib152","doi-asserted-by":"crossref","DOI":"10.1038\/nrd.2016.51","article-title":"Open Lab as a source of hits and leads against tuberculosis, malaria and kinetoplastid diseases","volume":"15","author":"Ballell","year":"2016","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2018.03.020_bib153","series-title":"R&D Pipeline for Tuberculosis","author":"IFPMA","year":"2017"},{"key":"10.1016\/j.ejmech.2018.03.020_bib154","unstructured":"ClinicalTrials.gov, in clinicaltrials.gov, accessed March 3, 2018."},{"key":"10.1016\/j.ejmech.2018.03.020_bib155","doi-asserted-by":"crossref","first-page":"503","DOI":"10.1016\/j.drudis.2016.09.010","article-title":"Identification and validation of novel drug targets in Mycobacterium tuberculosis","volume":"22","author":"Singh","year":"2017","journal-title":"Drug Discov. 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