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3-甲酰基色酮:具有潜在抗炎作用的化合物。

3-Formylchromones: potential antiinflammatory agents.

机构信息

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.

出版信息

Eur J Med Chem. 2010 Sep;45(9):4058-64. doi: 10.1016/j.ejmech.2010.05.065. Epub 2010 Jun 8.

Abstract

The synthesis and characterization of 3-formylchromone (1) and its derivatives 2-24 and evaluation of their potential antiinflammatory activities is reported here. These compounds were characterized by (1)H NMR, EI MS, IR, and UV spectroscopic techniques and elemental analysis. The synthesized compounds were evaluated by using various in vitro and in vivo assay models for antiinflammatory activity and their effects were compared with known standard drug such as aspirin and indomethacin. Among all tested compounds, 1, 2, 5, 6, 9, 14, 16-19, 21-23, showed promising antiinflammatory activities. The results and SAR has been discussed in this report.

摘要

本文报道了 3-甲酰基色酮(1)及其衍生物 2-24 的合成与表征,并评估了它们潜在的抗炎活性。这些化合物通过(1)H NMR、EI MS、IR 和 UV 光谱技术以及元素分析进行了表征。通过使用各种体外和体内抗炎活性测定模型对合成化合物进行了评估,并将其与已知标准药物如阿司匹林和吲哚美辛进行了比较。在所测试的所有化合物中,1、2、5、6、9、14、16-19、21-23 表现出有希望的抗炎活性。本文报告了结果和 SAR。

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