Structural Rigidification of N-Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorKings Coll London-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniv Cape Town-
Autor(es): dc.contributorUniv Siena-
Autor(es): dc.creatorSemenya, Dorothy-
Autor(es): dc.creatorTouitou, Meir-
Autor(es): dc.creatorRibeiro, Camila Maringolo [UNESP]-
Autor(es): dc.creatorPavan, Fernando Rogerio [UNESP]-
Autor(es): dc.creatorPisano, Luca-
Autor(es): dc.creatorSingh, Vinayak-
Autor(es): dc.creatorChibale, Kelly-
Autor(es): dc.creatorBano, Georg-
Autor(es): dc.creatorToscani, Anita-
Autor(es): dc.creatorManetti, Fabrizio-
Autor(es): dc.creatorGianibbi, Beatrice-
Autor(es): dc.creatorCastagnolo, Daniele-
Data de aceite: dc.date.accessioned2022-08-04T22:00:19Z-
Data de disponibilização: dc.date.available2022-08-04T22:00:19Z-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2022-01-12-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1021/acsmedchemlett.1c00431-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/218986-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/218986-
Descrição: dc.descriptionA series of indolyl-3-methyleneamines incorporating lipophilic side chains were designed through a structural rigidification approach and synthesized for investigation as new chemical entities against Mycobacterium tuberculosis (Mtb). The screening led to the identification of a 6-chloroindole analogue 7j bearing an N-octyl chain and a cycloheptyl moiety, which displayed potent in vitro activity against laboratory and clinical Mtb strains, including a pre-extensively drug-resistant (pre-XDR) isolate. 7j also demonstrated a marked ability to restrict the intracellular growth of Mtb in murine macrophages. Further assays geared toward mechanism of action elucidation have thus far ruled out the involvement of various known promiscuous targets, thereby suggesting that the new indole 7j may inhibit Mtb via a unique mechanism.-
Descrição: dc.descriptionSouth African National Research Foundation-SARChI-
Descrição: dc.descriptionUniversity of London-
Descrição: dc.descriptionSouth African Medical Research Council (SAMRC)-
Descrição: dc.descriptionSouth African Department of Science and Innovation-
Descrição: dc.descriptionSouth African National Research Foundation-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionKings Coll London, Sch Canc & Pharmaceut Sci, London SE1 9NH, England-
Descrição: dc.descriptionSao Paulo State Univ UNESP, TB Res Lab, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP, Brazil-
Descrição: dc.descriptionUniv Cape Town, Drug Discovery & Dev Ctr H3D, ZA-7701 Rondebosch, South Africa-
Descrição: dc.descriptionUniv Cape Town, South African Med Res Council Drug Discovery & De, Dept Chem, ZA-7701 Rondebosch, South Africa-
Descrição: dc.descriptionUniv Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa-
Descrição: dc.descriptionUniv Siena, Dipartimento Biotecnol Chim & Farm, I-53100 Siena, Italy-
Descrição: dc.descriptionSao Paulo State Univ UNESP, TB Res Lab, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP, Brazil-
Formato: dc.format63-69-
Idioma: dc.languageen-
Publicador: dc.publisherAmer Chemical Soc-
Relação: dc.relationAcs Medicinal Chemistry Letters-
???dc.source???: dc.sourceWeb of Science-
Palavras-chave: dc.subjectTuberculosis-
Palavras-chave: dc.subjectMDR-TB-
Palavras-chave: dc.subjectXDR-TB-
Palavras-chave: dc.subjectIndole-
Palavras-chave: dc.subjectPyrrole-
Palavras-chave: dc.subjectAntimicrobial resistance-
Título: dc.titleStructural Rigidification of N-Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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