Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria

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dc.contributor.authorTouitou, Meir
dc.contributor.authorManetti, Fabrizio
dc.contributor.authorRibeiro, Camila Maringolo [UNESP]
dc.contributor.authorPavan, Fernando Rogerio [UNESP]
dc.contributor.authorScalacci, Nicolò
dc.contributor.authorZrebna, Katarina
dc.contributor.authorBegum, Neelu
dc.contributor.authorSemenya, Dorothy
dc.contributor.authorGupta, Antima
dc.contributor.authorBhakta, Sanjib
dc.contributor.authorMchugh, Timothy D.
dc.contributor.authorSenderowitz, Hanoch
dc.contributor.authorKyriazi, Melina
dc.contributor.authorCastagnolo, Daniele
dc.contributor.institutionKing's College London
dc.contributor.institutionChimica e Farmacia
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversity College London
dc.contributor.institutionUniversity of London
dc.contributor.institutionBar-Ilan University
dc.date.accessioned2020-12-12T02:32:59Z
dc.date.available2020-12-12T02:32:59Z
dc.date.issued2020-05-14
dc.description.abstractA series of N-phenyl-2,5-dimethylpyrrole derivatives, designed as hybrids of the antitubercular agents BM212 and SQ109, have been synthesized and evaluated against susceptible and drug-resistant mycobacteria strains. Compound 5d, bearing a cyclohexylmethylene side chain, showed high potency against M. tuberculosis including MDR-TB strains at submicromolar concentrations. The new compound shows bacteriostatic activity and low toxicity and proved to be effective against intracellular mycobacteria too, showing an activity profile similar to isoniazid.en
dc.description.affiliationSchool of Cancer and Pharmaceutical Sciences King's College London, 150 Stamford Street
dc.description.affiliationDipartimento di Biotecnologie Chimica e Farmacia, via A. Moro 2
dc.description.affiliationTuberculosis Research Laboratory School of Pharmaceutical Sciences Sao Paulo State University (UNESP), Rod. Araraquara-Jau, km1
dc.description.affiliationCentre for Clinical Microbiology University College London
dc.description.affiliationMycobacteria Research Laboratory Department of Biological Sciences Institute of Structural and Molecular Biology Birkbeck University of London, Malet Street
dc.description.affiliationDepartment of Chemistry Faculty of Exact Sciences Bar-Ilan University
dc.description.affiliationUnespTuberculosis Research Laboratory School of Pharmaceutical Sciences Sao Paulo State University (UNESP), Rod. Araraquara-Jau, km1
dc.format.extent638-644
dc.identifierhttp://dx.doi.org/10.1021/acsmedchemlett.9b00515
dc.identifier.citationACS Medicinal Chemistry Letters, v. 11, n. 5, p. 638-644, 2020.
dc.identifier.doi10.1021/acsmedchemlett.9b00515
dc.identifier.issn1948-5875
dc.identifier.scopus2-s2.0-85077653042
dc.identifier.urihttp://hdl.handle.net/11449/201456
dc.language.isoeng
dc.relation.ispartofACS Medicinal Chemistry Letters
dc.sourceScopus
dc.subjectantimycobacterial drug
dc.subjectdrug resistance
dc.subjectintracellular tuberculosis
dc.subjectpyrroles
dc.subjectTuberculosis
dc.titleImproving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteriaen
dc.typeArtigo
unesp.author.orcid0000-0002-9598-2339[2]
unesp.author.orcid0000-0003-0076-1355[12]
unesp.author.orcid0000-0002-7517-5732[14]

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