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

Castagnolo, Daniele, de Logu, Alessandro, Radi, Marco, Bechi, Beatrice, Manetti, Fabrizio, Magnani, Matteo, Supino, Sibilla, Meleddu, Rita, Chisu, Lorenza and Botta, Maurizio (2008) Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis. Bioorganic & Medicinal Chemistry, 16 (18). pp. 8587-8591. ISSN 0968-0896

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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.

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