Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/337189
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dc.contributor.CRUESPUNIVERSIDADE ESTADUAL DE CAMPINASpt_BR
dc.contributor.authorunicampKoovits, Paul John-
dc.contributor.authorunicampDessoy, Marco Aurélio-
dc.contributor.authorunicampDias, Luiz Carlos-
dc.typeArtigopt_BR
dc.titleStructure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzipt_BR
dc.contributor.authorKoovits, Paul J.-
dc.contributor.authorDessoy, Marco A.-
dc.contributor.authorMatheeussen, An; Maes, Louis-
dc.contributor.authorCaljon, Guy-
dc.contributor.authorMowbray, Charles E.-
dc.contributor.authorKratz, Jadel M.-
dc.contributor.authorDias, Luiz C.-
dc.subjectDoença de Chagaspt_BR
dc.subject.otherlanguageChagas diseasept_BR
dc.description.abstractThe structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline's recently disclosed open-resource "Chagas box" and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chemistry efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discoverypt_BR
dc.relation.ispartofBioorganic and medicinal chemistry letterspt_BR
dc.relation.ispartofabbreviationBioorg. med. chem. lett.pt_BR
dc.publisher.cityOxfordpt_BR
dc.publisher.countryReino Unidopt_BR
dc.publisherElsevierpt_BR
dc.date.issued2020-
dc.date.monthofcirculationJan.pt_BR
dc.language.isoengpt_BR
dc.description.volume30pt_BR
dc.description.issuenumber1pt_BR
dc.rightsFechadopt_BR
dc.sourceWOSpt_BR
dc.identifier.issn0960-894Xpt_BR
dc.identifier.eissn1464-3405pt_BR
dc.identifier.doi10.1016/j.bmcl.2019.126779pt_BR
dc.identifier.urlhttps://www.sciencedirect.com/science/article/pii/S0960894X19307449pt_BR
dc.description.sponsorshipFAPESP – Fundação de Amparo à Pesquisa Do Estado De São Paulopt_BR
dc.description.sponsordocumentnumber2015/19495-5; 2015/50655-9; 2013/07600-3pt_BR
dc.date.available2020-03-23T17:28:42Z-
dc.date.accessioned2020-03-23T17:28:42Z-
dc.description.provenanceSubmitted by Sanches Olivia (olivias@unicamp.br) on 2020-03-23T17:28:42Z No. of bitstreams: 0en
dc.description.provenanceMade available in DSpace on 2020-03-23T17:28:42Z (GMT). No. of bitstreams: 0 Previous issue date: 2020en
dc.identifier.urihttp://repositorio.unicamp.br/jspui/handle/REPOSIP/337189-
dc.contributor.departmentsem informaçãopt_BR
dc.contributor.departmentsem informaçãopt_BR
dc.contributor.departmentDepartamento de Química Orgânicapt_BR
dc.contributor.unidadeInstituto de Químicapt_BR
dc.contributor.unidadeInstituto de Químicapt_BR
dc.contributor.unidadeInstituto de Químicapt_BR
dc.subject.keywordNeglected diseasespt_BR
dc.subject.keywordDrug discoverypt_BR
dc.subject.keywordAzaindolept_BR
dc.identifier.source000499694600015pt_BR
dc.creator.orcid0000-0002-8435-9437pt_BR
dc.creator.orcidsem informaçãopt_BR
dc.creator.orcid0000-0003-0628-9928pt_BR
dc.type.formArtigo de Periódicopt_BR
dc.identifier.articleid126779pt_BR
dc.description.sponsorNoteWe would like to thank FAPESP (Grant Nos 2015/19495-5, 2015/50655-9 and 2013/07600-3) as well as DNDi for funding; UNICAMP NMR and technical staff for assistance; The Thomson Mass Spectrometry Lab at UNICAMP for use of HRMS equipment; the High-Throughput ADME team at AbbVie for ADME testing; and additional thanks to Sir Simon Campbell, Dr. Dale Kempf (AbbVie), and Dr. Michael Schrimpf (AbbVie) for helpful discussions. DNDi is grateful to its donors, public and private, who have provided funding for all DNDi activities since its inception in 2003. A full list of DNDi’s donors can be found at http://www.dndi.org/donors/donors/pt_BR
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