Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis

Daniele Castagnolo, Alessandro de Logu, Marco Radi, Beatrice Bechi, Fabrizio Manetti, Matteo Magnani, Sibilla Supino, Rita Meleddu, Lorenza Chisu, Maurizio Botta

Research output: Contribution to journalArticlepeer-review

111 Citations (Scopus)
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Abstract

As a continuation of our previous work that turned toward the identification of antimycobacterial compounds with innovative structures, two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis (MTB), which is the causative agent of tuberculosis. One of these compounds showed high activity against MTB (MIC = 4 μg/mL). The newly synthesized pyrazoles were also computationally investigated to analyze their fit properties to the pharmacophoric model for antitubercular compounds previously built by us and to refine structure–activity relationship analysis.
Original languageEnglish
Pages (from-to)8587-8591
JournalBioorganic & Medicinal Chemistry
Volume16
Issue number18
DOIs
Publication statusPublished - 2008

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