Yu Juanhong, Tang Lei, Yang Yushe, Ji Ruyun
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Graduate School of the Chinese Academy of Sciences, CAS, Shanghai 201203, China.
Eur J Med Chem. 2008 Nov;43(11):2428-35. doi: 10.1016/j.ejmech.2008.01.029. Epub 2008 Feb 2.
A series of benzopyran derivatives were synthesized and evaluated for PPAR alpha/gamma agonist activities. Most of the compounds exhibit reasonable PPAR alpha and PPAR gamma agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPARg EC(50) values of 0.001microM are excellent full PPAR gamma agonists with the functional potency about 130, 20 times stronger than that of leading compound 5 and rosiglitazone, respectively. Compounds 7a, 7c, 7d and 8a are dual PPAR alpha/gamma agonists, and all of them gave comparable or stronger PPAR alpha/gamma agonist efficacy than that of the corresponding positive control.
合成了一系列苯并吡喃衍生物，并对其过氧化物酶体增殖物激活受体α/γ激动剂活性进行了评估。大多数化合物表现出合理的过氧化物酶体增殖物激活受体α和过氧化物酶体增殖物激活受体γ激动剂活性。特别是，化合物7b、8b、8e和8h具有显著的过氧化物酶体增殖物激活受体γ半数有效浓度（EC50）值，为0.001微摩尔，是出色的完全过氧化物酶体增殖物激活受体γ激动剂，其功能效力分别比先导化合物5和罗格列酮强约130倍、20倍。化合物7a、7c、7d和8a是双过氧化物酶体增殖物激活受体α/γ激动剂，它们均表现出与相应阳性对照相当或更强的过氧化物酶体增殖物激活受体α/γ激动剂效力。
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