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

被引：132

作者：

Castagnolo, Daniele ^{[1
]}

De Logu, Alessandro ^{[2
]}

Radi, Marco ^{[1
]}

Bechi, Beatrice ^{[1
]}

Manetti, Fabrizio ^{[1
]}

Magnani, Matteo ^{[1
]}

Supino, Sibilla ^{[1
]}

Meleddu, Rita ^{[2
]}

Chisu, Lorenza ^{[2
]}

Botta, Maurizio ^{[1
]}

机构：

[1] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy

[2] Univ Cagliari, Sez Microbiol Med, Dipartimento Sci & Tecnol Biomed, I-09123 Cagliari, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 18期

关键词：

tuberculosis; 5-hydroxy-pyrazole; pyrazolone; SAR study;

D O I：

10.1016/j.bmc.2008.08.016

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu g/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 re. ne structure-activity relationship analysis. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：8587 / 8591

页数：5

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