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

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Autor(es): dc.contributorKing's College London-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversity of Cape Town-
Autor(es): dc.contributorUniversità di Siena-
Autor(es): dc.creatorSemenya, Dorothy-
Autor(es): dc.creatorTouitou, Meir-
Autor(es): dc.creatorRibeiro, Camila Maringolo-
Autor(es): dc.creatorPavan, Fernando Rogerio-
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.accessioned2025-08-21T20:58:36Z-
Data de disponibilização: dc.date.available2025-08-21T20:58:36Z-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2022-05-01-
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/11449/233891-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/233891-
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.descriptionSchool of Cancer and Pharmaceutical Sciences King's College London, 150 Stamford Street-
Descrição: dc.descriptionTuberculosis Research Laboratory School of Pharmaceutical Sciences Sao Paulo State University (UNESP), Rodovia Araraquara-Jau, km1-
Descrição: dc.descriptionDrug Discovery and Development Centre (H3D) University of Cape Town-
Descrição: dc.descriptionSouth African Medical Research Council Drug Discovery and Development Research Unit Department of Chemistry Institute of Infectious Disease and Molecular Medicine University of Cape Town-
Descrição: dc.descriptionDipartimento di Biotecnologie Chimica e Farmacia Università di Siena, via Aldo Moro 2-
Descrição: dc.descriptionTuberculosis Research Laboratory School of Pharmaceutical Sciences Sao Paulo State University (UNESP), Rodovia Araraquara-Jau, km1-
Formato: dc.format63-69-
Idioma: dc.languageen-
Relação: dc.relationACS Medicinal Chemistry Letters-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectAntimicrobial resistance-
Palavras-chave: dc.subjectIndole-
Palavras-chave: dc.subjectMDR-TB-
Palavras-chave: dc.subjectPyrrole-
Palavras-chave: dc.subjectTuberculosis-
Palavras-chave: dc.subjectXDR-TB-
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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