Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 15, Pages 5716-5721Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.05.058
Keywords
Tuberculosis; Pyrazolones; Pyrazole; SAR study
Funding
- Italian Ministero dell'Istruzione, dell'Universita e della Ricerca [PRIN 2005037820]
- CARIPLO [2006.0880/10.8485 Bando 2006]
- Asinex
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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 mu g/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. (C) 2009 Elsevier Ltd. All rights reserved.
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