Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5679
Title: Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: Part 2. Synthesis of rigid pyrazolones
Authors: Castagnolo, D
Manetti, Fabrizio 
Botta, Maurizio 
Bechi, B
Pagano, M
DE LOGU, A
Meleddu, R
Saddi, M
Botta, Maurizio 
Keywords: Pyrazole; Pyrazolones; SAR study; Tuberculosis
Issue Date: 2009
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis. Two of these compounds showed a high activity against MTB (MIC = 4 μg/mL). The newly synthesized pyrazolones were also computationally investigated to analyze if their properties fit the pharmacophoric model for antitubercular compounds previously built by us. The results are in agreement with those reported by us previously for a class of pyrazole analogues and confirm the fundamental role of the p-chlorophenyl moiety at C4 in the antimycobacterial activity.
Description: 
25533
URI: http://hdl.handle.net/20.500.12779/5679
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2009.05.058
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