Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5763
Title: Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin
Authors: Biava, M
PORRETTA G., C
Poce, G
Battilocchio, C
Alfonso, S
DE LOGU, A
Serra, N
Manetti, Fabrizio 
Botta, Maurizio 
Keywords: Cytotoxicity; Pharmacophore model; Protection index; Pyrroles; Tuberculosis
Issue Date: 2010
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
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.
Description: 
25359
URI: http://hdl.handle.net/20.500.12779/5763
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2010.09.006
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