Syntheses and anti-inflammatory and analgesic activities of hydroxamic acids and acid hydrazides.
作者:KUNIYOSHI TANAKA、KEIZO MATSUO、AI NAKANISHI、TOSHIKO HATANO、HISAKO IZEKI、YOKO ISHIDA、WASUKE MORI
DOI:10.1248/cpb.31.2810
日期:——
On the basis of the generally accepted view that copper ions take part in the occurrence of inflammation, hydroxamic acids and acid hydrazides derived from various substituted cinnamic acids and hydrocinnamic acids, which were expected to chelate with copper ions, were synthesized and evaluated for anti-inflammatory activity by the carrageenin-induced rat paw edema assay and for analgesic activity by the phenylquinone writhing method in mice. Some of the synthesized compounds exhibited both activities, and 3-(3, 4-dimethoxyphenyl)propiohydroxamic acid and its Zn complex were more active than aspirin. The Cu (II) complexes of hydroxamic acid derivatives were synthesized and were assumed to have polymeric structures from the results of elemental analysis, molecular weight measurement and determination of magnetic susceptibility.
根据普遍接受的观点,铜离子参与了炎症的发生,因此合成了来自各种取代肉桂酸和氢肉桂酸的羟肟酸和酸肼,期望它们能与铜离子形成配位化合物,并通过卡拉胶诱导的大鼠爪肿胀实验评估其抗炎活性,通过苯醌扭动法评估其镇痛活性。部分合成的化合物表现出这两种活性,3-(3, 4-二甲氧基苯基)丙氢羟肟酸及其锌配合物的活性超过阿司匹林。羟肟酸衍生物的铜(II)配合物被合成,并根据元素分析、分子量测定和磁性测试结果推测其具有聚合结构。