作为镇痛和抗炎剂的4-取代吡啶并[2,3-d]嘧啶-4(1H)-酮的合成
Synthesis of 4-substituted pyrido[2,3-d]pyrimidin-4(1H)-one as analgesic and anti-inflammatory agents.
作者信息
El-Gazzar Abdel-Rahman B A, Hafez Hend N
机构信息
National Research Centre, Photochemistry Department (Heterocyclic and Nucleoside Unit), Dokki, Giza, 12622 Cairo, Egypt.
出版信息
Bioorg Med Chem Lett. 2009 Jul 1;19(13):3392-7. doi: 10.1016/j.bmcl.2009.05.044. Epub 2009 May 18.
4-Substituted-pyrido[2,3-d]pyrimidin-4(1H)-ones 4a-c were synthesized by oxidation of 4-substituted-dihydropyrido[2,3-d]pyrimidin-4(1H)-ones 3a-c which were in turn prepared from arylidenemalononitriles 1a-c and 6-aminothiouracil 2. The reactivity of compounds 4a-c towards some reagents such as formamide, carbon disulfide, urea, thiourea, formic and acetic acids were studied. All the synthesized compounds were characterized by spectroscopic means and elemental analysis. Compound 4c exhibited 64% and 72% analgesic activity. Also, compound 4b showed 50% and 65% anti-inflammatory activity. Interestingly these compounds showed one-third of ulcer index of the reference aspirin and diclofenac.
通过氧化4-取代的二氢吡啶并[2,3-d]嘧啶-4(1H)-酮3a-c合成了4-取代的吡啶并[2,3-d]嘧啶-4(1H)-酮4a-c，而3a-c又由芳基亚甲基丙二腈1a-c和6-氨基硫脲2制备。研究了化合物4a-c对一些试剂如甲酰胺、二硫化碳、尿素、硫脲、甲酸和乙酸的反应活性。所有合成的化合物都通过光谱手段和元素分析进行了表征。化合物4c表现出64%和72%的镇痛活性。此外，化合物4b表现出50%和65%的抗炎活性。有趣的是，这些化合物的溃疡指数仅为参比阿司匹林和双氯芬酸的三分之一。
Zotero 插件