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

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.

SUBMITTER: Touitou M

PROVIDER: S-EPMC7236041 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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

Touitou Meir M Manetti Fabrizio F Ribeiro Camila Maringolo CM Pavan Fernando Rogerio FR Scalacci Nicolò N Zrebna Katarina K Begum Neelu N Semenya Dorothy D Gupta Antima A Bhakta Sanjib S McHugh Timothy D TD Senderowitz Hanoch H Kyriazi Melina M Castagnolo Daniele D

ACS medicinal chemistry letters 20191210 5

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 intrac ...[more]

PMID: 32435364

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