Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria
- Touitou M.
- Manetti F.
- Ribeiro C. M.
- Pavan F. R.
- Scalacci N.
- Zrebna K.
- Begum N.
- Semenya D.
- Gupta A.
- Bhakta S.
- McHugh T. D.
- Senderowitz H.
- Kyriazi M.
- Castagnolo D.
Publication date
January 2020
DOI Publisher
American Chemical Society (ACS)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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