347331-67-3Relevant articles and documents
Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria
Touitou, Meir,Manetti, Fabrizio,Ribeiro, Camila Maringolo,Pavan, Fernando Rogerio,Scalacci, Nicolò,Zrebna, Katarina,Begum, Neelu,Semenya, Dorothy,Gupta, Antima,Bhakta, Sanjib,Mchugh, Timothy D.,Senderowitz, Hanoch,Kyriazi, Melina,Castagnolo, Daniele
, p. 638 - 644 (2020/01/11)
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.