Touitou, M;
Manetti, F;
Ribeiro, CM;
Pavan, FR;
Scalacci, N;
Zrebna, K;
Begum, N;
... Castagnolo, D; + view all
(2020)
Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria.
ACS Medicinal Chemistry Letters
, 11
(5)
pp. 638-644.
10.1021/acsmedchemlett.9b00515.
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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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