Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist

Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist
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微小的结构修饰将选择性 PPARα 激动剂转化为有效的、高选择性 PPARδ 激动剂

DOI:
10.1016/j.bmcl.2005.06.023
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发表时间:
2005
影响因子:
2.7
通讯作者:
Michael Woltering
Michael Woltering
中科院分区:
医学4区
文献类型:
--
作者:
S. Weigand;H. Bischoff;Elke Dittrich;H. Heckroth;D. Lang;Andrea Vaupel;Michael Woltering

文献摘要

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我们报道了一系列新的人过氧化物酶体增殖物激活受体δ(PPARδ)的小分子激动剂的固相合成和药理学评价。化合物33显示出良好的药代动力学。
We report the solid-phase synthesis and pharmacological evaluation of a new series of small-molecule agonists of the human peroxisome proliferator-activated receptor δ (PPARδ) based on a lead structure from our PPARα program. Compound 33 showed good pharmacokinetics.