Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates
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DOI：
10.1016/j.bmc.2010.06.002
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发表时间：
2010-07-15
影响因子：
3.5
通讯作者：
Alexandre-Moreira, Magna Suzana
中科院分区：
文献类型：
--
作者：
Cupertino da Silva, Yolanda Karla;Augusto, Cristina Villarinho;Alexandre-Moreira, Magna Suzana
在本文中，我们报道了吡嗪N-酰腙（NAH）衍生物（2a-s）的合成和药理学评价，该衍生物被设计为新型镇痛和抗炎候选药物。该系列是通过原型 1 (LASSBio-1018) 的分子简化而设计的，原型 1 先前被描述为非选择性环氧合酶抑制剂。衍生物 2a-s 在多种疼痛和炎症动物模型中进行了评估，其中突出的化合物 2o (2-N'-[(E)-(3,4,5-三甲氧基苯基)亚甲基]-2-吡嗪碳酰肼；LASSBio-1181) 在慢性炎症小鼠模型（即大鼠佐剂诱导关节炎试验）中也具有活性，可被视为一种新的镇痛药和镇痛药。药物开发的抗炎先导。由爱思唯尔有限公司出版
In this paper, we report the synthesis and pharmacological evaluation of pyrazine N-acylhydrazone (NAH) derivatives (2a-s) designed as novel analgesic and anti-inflammatory drug candidates. This series was planned by molecular simplification of prototype 1 (LASSBio-1018), previously described as a nonselective cyclooxygenase inhibitor. Derivatives 2a-s were evaluated in several animal models of pain and inflammation, standing-out compound 2o (2-N'-[(E)-(3,4,5-trimethoxyphenyl) methylidene]-2-pyrazinecarbohydrazide; LASSBio-1181), that was also active in a murine model of chronic inflammation (i.e., adjuvant-induced arthritis test in rats) and can be considered a new analgesic and anti-inflammatory lead for drug development. Published by Elsevier Ltd.