含吡啶的二芳醚类化合物的合成及其PDE4B抑制活性  

Synthesis and phosphodiesterase 4B inhibitory activities of diaryl ether derivatives containing pyridine

作　　者：李欣 王永强 袁威[1] 赵新筠[1] 张展 陈喜[1] LI Xin;WANG Yongqiang;YUAN Wei;ZHAO Xinyun;ZHANG Zhan;CHEN Xi(College of Chemistry and Material Science,South-Central Minzu University,Wuhan 430074,China)

机构地区：[1]中南民族大学化学与材料科学学院,武汉430074

出　　处：《中南民族大学学报（自然科学版）》2023年第4期441-449,共9页Journal of South-Central University for Nationalities：Natural Science Edition

基　　金：国家自然科学基金资助项目(21273089)。

摘　　要：磷酸二酯酶4B(PDE4B)是抗炎药物作用的重要靶标,以三嗪类PDE4B抑制剂A33为先导化合物,设计并合成了20个二芳醚类化合物.用1H NMR、^(13)C NMR等对化合物进行了结构表征,并对这些化合物进行了PDE4B抑制活性测试.结果表明:化合物3和4a表现出较好的PDE4B抑制活性,展现出它们作为进一步优化和开发更有效PDE4B抑制剂的先导化合物的潜力.Phosphodiesterase 4B(PDE4B)is a crucial therapeutic target for developing anti-inflammatory drugs.20 diaryl ether derivatives were synthesized using the PDE4B inhibitor A33 as a lead compound.The synthesized compounds were characterized using various techniques,including 1H and ^(13)C NMR spectroscopy.Subsequently,their inhibitory activities against PDE4B were evaluated.The results indicated that compounds 3 and 4a possessed promising inhibitory activities against the PDE4B enzyme,highlighting their potential as lead compounds for further optimization and development of more potent PDE4B inhibitors.

关 键 词：PDE4B抑制剂 二芳醚类化合物 合成 生物活性测试 

分 类 号：O625.6[理学—有机化学]