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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
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Touitou, Meir [1] ; Manetti, Fabrizio [2] ; Ribeiro, Camila Maringolo [3] ; Pavan, Fernando Rogerio [3] ; Scalacci, Nicolo [1] ; Zrebna, Katarina [1] ; Begum, Neelu [4] ; Semenya, Dorothy [1] ; Gupta, Antima [5, 6] ; Bhakta, Sanjib [5] ; McHugh, Timothy D. [4] ; Senderowitz, Hanoch [7] ; Kyriazi, Melina [1] ; Castagnolo, Daniele [1]
Total Authors: 14
Affiliation:
[1] Kings Coll London, Sch Canc & Pharmaceut Sci, 150 Stamford St, London SE1 9NH - England
[2] Dipartimento Biotecnol Chim & Farm, Via A Moro 2, I-53100 Siena - Italy
[3] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, TB Res Lab, Rod Araraquara Jau, Km1, BR-14800903 Araraquara, SP - Brazil
[4] UCL, Ctr Clin Microbiol, London NW3 2PF - England
[5] Birkbeck Univ London, Inst Struct & Mol Biol, Dept Biol Sci, Mycobacteria Res Lab, Malet St, London WC1E 7HX - England
[6] London Sch Hyg & Trop Med, Fac Infect Dis, London WC1E 7HT - England
[7] Bar Ilan Univ, Fac Exact Sci, Dept Chem, IL-5290002 Ramat Gan - Israel
Total Affiliations: 7
Document type: Journal article
Source: ACS Medicinal Chemistry Letters; v. 11, n. 5, p. 638-644, MAY 14 2020.
Web of Science Citations: 0
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. (AU)

FAPESP's process: 18/00163-0 - Development and search of new antimicrobials against Tuberculosis: from screening to pre-clinical studies in vivo
Grantee:Fernando Rogério Pavan
Support Opportunities: Regular Research Grants