King's College London

Research portal

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

Research output: Contribution to journalArticle

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

Original languageEnglish
Pages (from-to)638-644
Number of pages7
JournalAcs Medicinal Chemistry Letters
Volume11
Issue number5
DOIs
Published14 May 2020

King's Authors

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.

View graph of relations

© 2020 King's College London | Strand | London WC2R 2LS | England | United Kingdom | Tel +44 (0)20 7836 5454