TY - JOUR
T1 - Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria
AU - Touitou, Meir
AU - Manetti, Fabrizio
AU - Ribeiro, Camila Maringolo
AU - Pavan, Fernando Rogerio
AU - Scalacci, Nicolò
AU - Zrebna, Katarina
AU - Begum, Neelu
AU - Semenya, Dorothy
AU - Gupta, Antima
AU - Bhakta, Sanjib
AU - McHugh, Timothy D.
AU - Senderowitz, Hanoch
AU - Kyriazi, Melina
AU - Castagnolo, Daniele
PY - 2020/5/14
Y1 - 2020/5/14
N2 - 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.
AB - 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.
KW - antimycobacterial drug
KW - drug resistance
KW - intracellular tuberculosis
KW - pyrroles
KW - Tuberculosis
UR - http://www.scopus.com/inward/record.url?scp=85077653042&partnerID=8YFLogxK
U2 - 10.1021/acsmedchemlett.9b00515
DO - 10.1021/acsmedchemlett.9b00515
M3 - Article
AN - SCOPUS:85077653042
SN - 1948-5875
VL - 11
SP - 638
EP - 644
JO - Acs Medicinal Chemistry Letters
JF - Acs Medicinal Chemistry Letters
IS - 5
ER -
