A hit optimization procedure based on isosteric and bioisosteric replacement of decorating groups at both the N1 and the C5 phenyl rings of 1,5-diarylpyrroles led to identification of 4-((1-(4-fluorophenyl)-2-methyl-5- (4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine that is characterized by a very high activity toward both Mycobacterium tuberculosis 103471 and H37Rv strains (MIC values of 0.125 μg/mL), and a safe profile in terms of cytotoxicity (CC50 of >128 μg/mL) and protection index (>1000). Antitubercular activity and protection index of the new compound are comparable to those found for the current antitubercular drugs streptomycin and rifampin.
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|Titolo:||Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin|
|Rivista:||BIOORGANIC & MEDICINAL CHEMISTRY|
|Citazione:||Biava, M., PORRETTA G., C., Poce, G., Battilocchio, C., Alfonso, S., DE LOGU, A., et al. (2010). Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin. BIOORGANIC & MEDICINAL CHEMISTRY, 18(22), 8076-8084.|
|Appare nelle tipologie:||1.1 Articolo in rivista|