{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,31]],"date-time":"2026-10-31T00:59:46Z","timestamp":1793408386798,"version":"4.5.0"},"reference-count":33,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2017,2,1]],"date-time":"2017-02-01T00:00:00Z","timestamp":1485907200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"}],"funder":[{"DOI":"10.13039\/501100000704","name":"Royal Society of Chemistry","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100000704","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Birkbeck Anniversary\/Wellcome Trust"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2017,2]]},"DOI":"10.1016\/j.ejmech.2016.12.042","type":"journal-article","created":{"date-parts":[[2016,12,23]],"date-time":"2016-12-23T15:47:20Z","timestamp":1482508040000},"page":"147-158","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":30,"special_numbering":"C","title":["Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis"],"prefix":"10.1016","volume":"127","author":[{"given":"Nicol\u00f2","family":"Scalacci","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alistair K.","family":"Brown","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fernando R.","family":"Pavan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Camila M.","family":"Ribeiro","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fabrizio","family":"Manetti","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sanjib","family":"Bhakta","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Arundhati","family":"Maitra","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Darren L.","family":"Smith","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elena","family":"Petricci","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Daniele","family":"Castagnolo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2016.12.042_bib1","unstructured":"http:\/\/www.who.int\/tb\/publications\/global_report\/en\/."},{"key":"10.1016\/j.ejmech.2016.12.042_bib2","doi-asserted-by":"crossref","first-page":"e17601","DOI":"10.1371\/journal.pone.0017601","article-title":"Natural history of tuberculosis: duration and fatality of untreated pulmonary tuberculosis in HIV negative patients: a systematic review","volume":"6","author":"Tiemersma","year":"2011","journal-title":"PLoS One"},{"key":"10.1016\/j.ejmech.2016.12.042_bib3","first-page":"268","article-title":"Interaction between HIV and Mycobacterium tuberculosis: HIV-1-induced CD4 T-cell depletion and the development of active tuberculosis","volume":"7","author":"Geldmacher","year":"2012","journal-title":"Curr. Opin. HIV AIDS"},{"key":"10.1016\/j.ejmech.2016.12.042_bib4a","doi-asserted-by":"crossref","first-page":"e0135802","DOI":"10.1371\/journal.pone.0135802","article-title":"Patient and provider reported reasons for lost to follow up in MDRTB treatment: a qualitative study from a drug resistant TB Centre in India","volume":"10","author":"Deshmukh","year":"2015","journal-title":"PLoS One"},{"key":"10.1016\/j.ejmech.2016.12.042_bib4b","first-page":"1","article-title":"Early diagnosis and effective treatment regimens are the keys to tackle antimicrobial resistance in tuberculosis (TB): a report from Euroscicon's international TB Summit 2016","author":"Maitra","year":"2016","journal-title":"Virulence"},{"key":"10.1016\/j.ejmech.2016.12.042_bib5","first-page":"829","article-title":"Treatment of multidrug-resistant tuberculosis:evidence and controversies","volume":"10","author":"Caminero","year":"2006","journal-title":"Int. J. Tuberc. Lung Dis."},{"key":"10.1016\/j.ejmech.2016.12.042_bib6","doi-asserted-by":"crossref","first-page":"1103","DOI":"10.1164\/rccm.200308-1159OC","article-title":"Treatment and outcome analysis of 205 patients with multidrug-resistant tuberculosis","volume":"169","author":"Chan","year":"2004","journal-title":"Am. J. Respir. Crit. Care Med."},{"key":"10.1016\/j.ejmech.2016.12.042_bib7","doi-asserted-by":"crossref","first-page":"1700","DOI":"10.3201\/eid1411.080729","article-title":"Multidrug- and extensively drug-resistant tuberculosis","volume":"14","author":"Eker","year":"2008","journal-title":"Emerg. Infect. Dis."},{"key":"10.1016\/j.ejmech.2016.12.042_bib8","doi-asserted-by":"crossref","first-page":"563","DOI":"10.1056\/NEJMoa0800106","article-title":"Comprehensive treatment of extensively drug-resistant tuberculosis","volume":"359","author":"Mitnick","year":"2008","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2016.12.042_bib9","first-page":"307","article-title":"The totally drug resistant tuberculosis (TDR-TB)","volume":"6","author":"Velayati","year":"2013","journal-title":"Int. J. Clin. Exp. Med."},{"key":"10.1016\/j.ejmech.2016.12.042_bib10","doi-asserted-by":"crossref","first-page":"2028","DOI":"10.1093\/jac\/dkv054","article-title":"Bactericidal mode of action of bedaquiline","volume":"70","author":"Hards","year":"2014","journal-title":"J.\u00a0Antimicrob. Chemother."},{"key":"10.1016\/j.ejmech.2016.12.042_bib11","doi-asserted-by":"crossref","first-page":"1984","DOI":"10.2146\/ajhp130199","article-title":"A\u00a0review of tuberculosis: focus on bedaquiline","volume":"70","author":"Chan","year":"2013","journal-title":"Am. J. Heal. Pharm."},{"key":"10.1016\/j.ejmech.2016.12.042_bib12","doi-asserted-by":"crossref","first-page":"968","DOI":"10.1093\/jac\/dki319","article-title":"Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines","volume":"56","author":"Protopopova","year":"2005","journal-title":"J.\u00a0Antimicrob. Chemother."},{"key":"10.1016\/j.ejmech.2016.12.042_bib13","doi-asserted-by":"crossref","first-page":"e12","DOI":"10.1038\/emi.2016.12","article-title":"Moxifloxacin and gatifloxacin for initial therapy of tuberculosis: a meta-analysis of randomized clinical trials","volume":"5","author":"Ruan","year":"2016","journal-title":"Emerg. Microbes Infect."},{"key":"10.1016\/j.ejmech.2016.12.042_bib14","doi-asserted-by":"crossref","first-page":"1508","DOI":"10.1056\/NEJMoa1201964","article-title":"Linezolid for treatment of chronic extensively drug-resistant tuberculosis","volume":"367","author":"Lee","year":"2012","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2016.12.042_bib15","doi-asserted-by":"crossref","first-page":"0006914","DOI":"10.1371\/journal.pone.0006914","article-title":"Treatment outcomes of multidrug-resistant tuberculosis: a systematic review and meta-analysis","volume":"4","author":"Johnston","year":"2009","journal-title":"PLoS One"},{"key":"10.1016\/j.ejmech.2016.12.042_bib16","doi-asserted-by":"crossref","first-page":"887","DOI":"10.2174\/138945006777709539","article-title":"\u201cNon-Antibiotics\u201d: alternative therapy for the management of MDRTB and MRSA in economically disadvantaged countries","volume":"7","author":"Amaral","year":"2006","journal-title":"Curr. Drug Targets"},{"key":"10.1016\/j.ejmech.2016.12.042_bib17","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1134\/S0026893310040096","article-title":"Identification of wild-type Mycobacterium tuberculosis isolates and point mutations associated with isoniazid resistance","volume":"44","author":"Limanskaya","year":"2010","journal-title":"Mol. Biol."},{"key":"10.1016\/j.ejmech.2016.12.042_bib18","doi-asserted-by":"crossref","first-page":"505","DOI":"10.1093\/jac\/47.5.505","article-title":"Activity of phenothiazines against antibiotic-resistant Mycobacterium tuberculosis: a review supporting further studies that may elucidate the potential use of thioridazine as anti-tuberculosis therapy","volume":"47","author":"Amaral","year":"2001","journal-title":"J.\u00a0Antimicrob. Chemother."},{"key":"10.1016\/j.ejmech.2016.12.042_bib19","doi-asserted-by":"crossref","first-page":"1021","DOI":"10.3390\/ph5091021","article-title":"Why and how the old neuroleptic thioridazine cures the XDR-TB patient","volume":"5","author":"Amaral","year":"2012","journal-title":"Pharm. (Basel)"},{"key":"10.1016\/j.ejmech.2016.12.042_bib20","first-page":"231","article-title":"Potential therapy of multidrug-resistant and extremely drug-resistant tuberculosis with thioridazine","volume":"26","author":"Amaral","year":"2012","journal-title":"Vivo (Brooklyn)"},{"key":"10.1016\/j.ejmech.2016.12.042_bib21","doi-asserted-by":"crossref","first-page":"35","DOI":"10.1186\/1471-2180-11-35","article-title":"Ethidium bromide transport across Mycobacterium smegmatis cell-wall: correlation with antibiotic resistance","volume":"11","author":"Rodrigues","year":"2011","journal-title":"BMC Microbiol."},{"key":"10.1016\/j.ejmech.2016.12.042_bib22","doi-asserted-by":"crossref","first-page":"0034538","DOI":"10.1371\/journal.pone.0034538","article-title":"Contribution of efflux to the emergence of isoniazid and multidrug resistance in Mycobacterium tuberculosis","volume":"7","author":"Machado","year":"2012","journal-title":"PLoS One"},{"key":"10.1016\/j.ejmech.2016.12.042_bib23","doi-asserted-by":"crossref","first-page":"1776","DOI":"10.1021\/acs.jproteome.5b01037","article-title":"Thioridazine alters the cell-envelope permeability of Mycobacterium tuberculosis","volume":"15","author":"de Keijzer","year":"2016","journal-title":"J.\u00a0Proteome Res."},{"key":"10.1016\/j.ejmech.2016.12.042_bib24","doi-asserted-by":"crossref","first-page":"338","DOI":"10.1016\/j.ijantimicag.2006.10.013","article-title":"In\u00a0vitro and ex\u00a0vivo activity of thioridazine derivatives against Mycobacterium tuberculosis","volume":"29","author":"Martins","year":"2007","journal-title":"Int. J. Antimicrob. Agents"},{"key":"10.1016\/j.ejmech.2016.12.042_bib25","doi-asserted-by":"crossref","first-page":"10384","DOI":"10.1002\/anie.201304290","article-title":"Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase","volume":"52","author":"Schlauderer","year":"2013","journal-title":"Angew. Chem. Int. Ed."},{"key":"10.1016\/j.ejmech.2016.12.042_bib26","doi-asserted-by":"crossref","first-page":"5842","DOI":"10.1021\/acs.jmedchem.5b00428","article-title":"Rational design and synthesis of thioridazine analogues as enhancers of the antituberculosis therapy","volume":"58","author":"Pieroni","year":"2015","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2016.12.042_bib27","doi-asserted-by":"crossref","first-page":"2780","DOI":"10.1021\/acs.jmedchem.6b00031","volume":"59","author":"Bhakta","year":"2016","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2016.12.042_bib28","doi-asserted-by":"crossref","first-page":"583","DOI":"10.1021\/ic50193a012","article-title":"Cation radicals of phenothiazines. Electron transfer with aquoiron(II) and -(III) and hexacyanoferrate(II) and -(III)","volume":"18","author":"Pelizzetti","year":"1979","journal-title":"Inorg. Chem."},{"key":"10.1016\/j.ejmech.2016.12.042_bib29","doi-asserted-by":"crossref","first-page":"456","DOI":"10.1016\/j.biopha.2011.04.021","article-title":"Drug resistance in Mycobacterium tuberculosis clinical isolates from Brazil: phenotypic and genotypic methods","volume":"65","author":"Miyata","year":"2011","journal-title":"Biomed. Pharmacother."},{"key":"10.1016\/j.ejmech.2016.12.042_bib30","doi-asserted-by":"crossref","first-page":"2720","DOI":"10.1128\/AAC.46.8.2720-2722.2002","article-title":"Resazurin microtiter assay Plate: simple and inexpensive method for detection of drug resistance in Mycobacterium tuberculosis","volume":"46","author":"Palomino","year":"2002","journal-title":"Antimicrob. Agents Chemother."},{"key":"10.1016\/j.ejmech.2016.12.042_bib31","doi-asserted-by":"crossref","first-page":"5421","DOI":"10.1046\/j.1432-1327.2000.01606.x","article-title":"Investigation of the Alamar Blue (resazurin) fluorescent dye for the assessment of mammalian cell cytotoxicity","volume":"267","author":"O'Brien","year":"2000","journal-title":"Eur. J. Biochem."},{"key":"10.1016\/j.ejmech.2016.12.042_bib32","doi-asserted-by":"crossref","first-page":"1898","DOI":"10.1016\/j.ejmech.2010.01.028","article-title":"Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide\/hydrazones: anti-Mycobacterium tuberculosis activity and cytotoxicity","volume":"45","author":"Pavan","year":"2010","journal-title":"Eur. J. Med. Chem."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523416310480?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523416310480?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2022,7,19]],"date-time":"2022-07-19T20:51:04Z","timestamp":1658263864000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523416310480"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2017,2]]},"references-count":33,"alternative-id":["S0223523416310480"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2016.12.042","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2017,2]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2016.12.042","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2016 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}]}}