Medicinal chemistry of N-acylhydrazones: Novel lead-compounds of analgesic, antinflammatory and antithrombotic drugs.

被引：59
作者：
Barreiro, EJ [1 ]
Fraga, CAM [1 ]
Miranda, ALP [1 ]
Rodrigues, CR [1 ]
机构：
[1] Univ Fed Rio de Janeiro, Fac Farm, LASSBio, BR-21944190 Rio De Janeiro, Brazil
来源：
QUIMICA NOVA | 2002年 / 25卷 / 01期
关键词：
bioactive N-acythydrazones derivatives; antinflammatory; analgesic and antithrombotic properties; molecular hybridization and bioisosterism in drug; design;
D O I：
10.1590/S0100-40422002000100022
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization or aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e,g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compound, clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.
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收藏
页码：129 / 148
页数：20
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