Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis
| Autor: | Alessandro De Logu, Fabrizio Manetti, Sibilla Supino, L Chisu, Beatrice Bechi, Rita Meleddu, Maurizio Botta, Matteo Magnani, Marco Radi, Daniele Castagnolo |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Tuberculosis
Stereochemistry medicine.drug_class F100 Clinical Biochemistry Pyrazolone Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Pyrazole Antimycobacterial Biochemistry Chemical synthesis Mycobacterium tuberculosis chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Molecular Biology Biological evaluation Antibacterial agent biology Organic Chemistry medicine.disease biology.organism_classification chemistry Molecular Medicine Pyrazoles medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry. 16(18) |
| ISSN: | 1464-3391 0968-0896 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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