Novel N-aryl- and N-heteryl phenazine-1-carboxamides as potential agents for the treatment of infections sustained by drug-resistant and multidrug-resistant Mycobacterium tuberculosis.
We investigated the in vitro activity of a new class of N-aryl and N-heteryl phenazine-1-carboxamide derivatives against Mycobacterium tuberculosis H37Rv and against drug-resistant ATCC M. tuberculosis strains. The activity against M. tuberculosis in J774 macrophage cells was also investigated. In most cases, minimum inhibitory concentrations (MICs) ranging between 0.19 mg/L and 0.79 mg/L were found, and comparable MIC values were obtained against 26 susceptible and 5 drug-resistant clinical isolates. Several derivatives were shown to be effective in inhibiting the growth both of susceptible and resistant strains at comparable concentrations. Results obtained indicate that these compounds could represent a promising class of agents useful for the treatment of M. tuberculosis infections caused by drug-resistant strains.
De Logu
Alessandro
A
Department of Sciences and Biomedical Technologies, Division of Medical Microbiology, University of Cagliari, Cagliari, Italy. adelogu@unica.it
Palchykovska
Larisa H
LH
Kostina
Valentina H
VH
Sanna
Adriana
A
Meleddu
Rita
R
Chisu
Lorenza
L
Alexeeva
Inna V
IV
Shved
Anatoly D
AD
D000818:Animals; D000995:Antitubercular Agents / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D008264:Macrophages / Q000382:microbiology; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010619:Phenazines / Q000494:pharmacology*
D000995:Antitubercular Agents; D010619:Phenazines; C420923:phenazine-1-carboxamide