摘要
目的 研究吡咯并吡嗪酮类化合物的抗炎镇痛作用构效关系,寻找具有抗炎镇痛活性的新型吡嗪酮类化合物。方法 以2-甲基-3-苯基吡咯并吡嗪-1(2H)-酮化合物为母体,合成系列化合物。用二甲苯致小鼠耳肿胀法和醋酸致小鼠扭体法对所合成的目标化合物分别进行了抗炎和镇痛活性实验。结果 合成了11个目标化合物,经1H-NMR和MS确证其结构。小鼠实验表明,一些所合成的化合物具有一定的抗炎或镇痛作用。结论 化合物14抗炎镇痛活性较好,值得进一步研究。
Abstract
OBJECTIVE To study the structure-activity relationship (SAR) of pyrrolepyrazinones and search for novel nonsteroidal anti-inflammatory agents. METHODS A series of pyrrolepyrazinone derivatives were synthesized. Their anti-inflammatory and analgesic activities were evaluated by xylene-induced ear edema and acetic acid-induced writhing in mice, respectively. RESULTS Eleven new compounds were synthesized and confirmed by 1H-NMR and MS. Some of the target compounds showed anti-inflammatory and/or analgesic activities. CONCLUSION Compound 14, which shows desirable anti-inflammatory activity and analgesic activity can be regarded as a valuable compound for further study.
关键词
3-苯基-6-酰基吡咯吡嗪酮 /
制备 /
化学合成 /
吡咯并吡嗪酮 /
抗炎 /
镇痛
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Key words
pyrrolepyrazinone /
preparation /
chemical synthesis /
pyrrolepyrazinone /
anti -inflammation /
analgesia
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吴丽颖,宋宏锐,崔凯.
3-苯基-6-酰基吡咯吡嗪酮的合成及抗炎镇痛活性研究[J]. 中国药学杂志, 2013, 48(3): 224-227 https://doi.org/10.11669/cpj.2013.03.014
WU Li-ying, SONG Hong-rui,CUI Kai.
Synthesis of Pyrrolepyrazinones and Study on Their Anti-Inflammatory and Analgesic Activities[J]. Chinese Pharmaceutical Journal, 2013, 48(3): 224-227 https://doi.org/10.11669/cpj.2013.03.014
中图分类号:
R96
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参考文献
MORIMOTO A, WATANABLE T. Pyrrole lactam derivatives with antiprotozoa antitrichomonas blood sugar decreasing and gastric juice apoleptic activity. JP: 7427877, 1974.
PANG J Y, SUN G, FU D C. Synthesis and anti-inflammatory and analgesic activities of dihydropyrrolopyrazin-1-one. Chin J Med Chem(中国药物化学杂志), 2002, 12(2): 82-85.
FU D C. Synthesis, anti- inflammatory and analgesic activities of pyrrolepyrazinone and pyrrolooxazinone derivatives. . Shenyang:School of Pharmaceutical Engineering, Shenyang Pharmaxeutical University, 2002.
WANG F. Synthesis and anti-inflammatory and analgesic activities of pyrrolopyrazinone derivatives . Shenyang:School of Pharmaceutical Engineering, Shenyang Pharmaxeutical University, 2004.
WU L Y, MA H, WANG Y L, et al. The study on synthesis and anti- inflammatory and analgesic activities of pyrrolepyrazinone. Hebei Chem Eng Ind(河北化工), 2007, 30(9):21-23.
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脚注
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基金
唐山市科学技术研究与发展计划(11150205A-16)
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