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

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

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


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.

Original languageEnglish
Pages (from-to)638-644
Number of pages7
JournalACS Medicinal Chemistry Letters
Issue number5
StatePublished - 14 May 2020

Bibliographical note

Funding Information:
We gratefully acknowledge EPSRC (Global Challenges Competition King’s College London), Global Challenges Research Fund at Birkbeck, University of London and Royal Society (RG160870) for research funding and financial support. MT acknowledge King’s College London for a period of leave. DS acknowledges the South African National Research Foundation-SARChI for financial support. We gratefully acknowledge NC3Rs (National Centre for the Replacement, Refinement and Reduction of Animals in Research, NC/T001240/1) for financial support and Carolyn Lam and Simona di Blasio for their help and training on Galleria mellonella assays. FRP and CMR acknowledge Sao Paulo Research Foundation (FAPESP - grant 2018/00163-0) for financial support.

Publisher Copyright:
Copyright © 2019 American Chemical Society.


  • Tuberculosis
  • antimycobacterial drug
  • drug resistance
  • intracellular tuberculosis
  • pyrroles


Dive into the research topics of 'Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria'. Together they form a unique fingerprint.

Cite this