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  • Title: Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.
    Author: Castagnolo D, De Logu A, Radi M, Bechi B, Manetti F, Magnani M, Supino S, Meleddu R, Chisu L, Botta M.
    Journal: Bioorg Med Chem; 2008 Sep 15; 16(18):8587-91. PubMed ID: 18752962.
    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 microg/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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