具有抗炎和抗肿瘤特性的3-芳基-5-十五烷基-1,2,4-恶二唑的合成。
Synthesis of 3-aryl-5-decapentyl-1,2,4-oxadiazoles possessing antiinflammatory and antitumor properties.
作者信息
Bezerra Natércia M Miranda, De Oliveira Shalom P, Srivastava Rajendra M, Da Silva Joel R
机构信息
Departamento de Química Fundamental, Centro de Ciencias Exatas e de Natureza, Universidade Federal de Pernambuco, CEP 50740-540 Recife, PE, Brazil.
出版信息
Farmaco. 2005 Nov-Dec;60(11-12):955-60. doi: 10.1016/j.farmac.2005.08.003. Epub 2005 Oct 20.
A simple, convenient and straightforward synthesis of 3-aryl-1,2,4-oxadiazoles 4a-f from arylamidoximes 1a-f and palmitic acid 2 is described. Compounds 4a-f are non-lethal in mice at four times the therapeutic dose (i.p., LD50>1 g kg(-1) of the animals' body weight). These heterocycles have been found to possess antiinflammatory property similar to aspirin and ibuprofen. Three compounds, viz., 4a, d, e have also been evaluated for antitumor activity, where 4d exhibited an excellent activity comparable to lapachol.
描述了一种由芳基偕胺肟1a - f和棕榈酸2简单、便捷且直接合成3 - 芳基 - 1,2,4 - 恶二唑4a - f的方法。化合物4a - f在小鼠体内以治疗剂量的四倍（腹腔注射，半数致死量>1 g kg⁻¹动物体重）时无致死性。已发现这些杂环化合物具有与阿司匹林和布洛芬相似的抗炎特性。还对三种化合物，即4a、d、e进行了抗肿瘤活性评估，其中4d表现出与拉帕醇相当的优异活性。
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