Document Report Card
Basic Information
ID: ALA4613277
Journal: ACS Med Chem Lett
Title: Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria.
Authors: Touitou M, Manetti F, Ribeiro CM, Pavan FR, Scalacci N, Zrebna K, Begum N, Semenya D, Gupta A, Bhakta S, McHugh TD, Senderowitz H, Kyriazi M, Castagnolo D.
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.
CiteXplore: 32435364