Improving the Potency of <i>N</i>-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria.

Touitou, Meir; Manetti, Fabrizio; Ribeiro, Camila Maringolo; Pavan, Fernando Rogerio; Scalacci, Nicolò; Zrebna, Katarina; Begum, Neelu; Semenya, Dorothy; Gupta, Antima; Bhakta, Sanjib; McHugh, Timothy D; Senderowitz, Hanoch; Kyriazi, Melina; Castagnolo, Daniele

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

Touitou, Meir; Manetti, Fabrizio; Ribeiro, Camila Maringolo; Pavan, Fernando Rogerio; Scalacci, Nicolò; Zrebna, Katarina; Begum, Neelu; Semenya, Dorothy; Gupta, Antima; Bhakta, Sanjib; McHugh, Timothy D; Senderowitz, Hanoch; Kyriazi, Melina; Castagnolo, Daniele.

Afiliação

Touitou M; School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, London SE1 9NH, U.K.
Manetti F; Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University Ramat-Gan 5290002, Israel.
Ribeiro CM; Dipartimento di Biotecnologie, Chimica e Farmacia, via A. Moro 2, I-53100 Siena, Italy.
Pavan FR; Tuberculosis Research Laboratory, School of Pharmaceutical Sciences, Sao Paulo State University (UNESP), Rod. Araraquara-Jau, km1, 14800-903 Araraquara, Brazil.
Scalacci N; Tuberculosis Research Laboratory, School of Pharmaceutical Sciences, Sao Paulo State University (UNESP), Rod. Araraquara-Jau, km1, 14800-903 Araraquara, Brazil.
Zrebna K; School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, London SE1 9NH, U.K.
Begum N; School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, London SE1 9NH, U.K.
Semenya D; Centre for Clinical Microbiology, University College London, London NW3 2PF, U.K.
Gupta A; School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, London SE1 9NH, U.K.
Bhakta S; Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, U.K.
McHugh TD; Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, U.K.
Senderowitz H; Centre for Clinical Microbiology, University College London, London NW3 2PF, U.K.
Kyriazi M; Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University Ramat-Gan 5290002, Israel.
Castagnolo D; School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, London SE1 9NH, U.K.

ACS Med Chem Lett ; 11(5): 638-644, 2020 May 14.

Article em En | MEDLINE | ID: mdl-32435364

ABSTRACT

ABSTRACT

A 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.

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Reino Unido País de publicação: EEUU / ESTADOS UNIDOS / ESTADOS UNIDOS DA AMERICA / EUA / UNITED STATES / UNITED STATES OF AMERICA / US / USA

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