一系列新型咪唑并[1,2-a]吡啶衍生物作为缺氧诱导因子-1α脯氨酰羟化酶抑制剂
A novel series of imidazo[1,2-a]pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
作者信息
Warshakoon Namal C, Wu Shengde, Boyer Angelique, Kawamoto Richard, Sheville Justin, Renock Sean, Xu Kevin, Pokross Matthew, Evdokimov Artem G, Walter Richard, Mekel Marlene
机构信息
Procter and Gamble Pharmaceuticals, Inc., 8700 Mason-Montgomery Road, Mason, OH 45040, USA.
出版信息
Bioorg Med Chem Lett. 2006 Nov 1;16(21):5598-601. doi: 10.1016/j.bmcl.2006.08.089. Epub 2006 Sep 8.
Utilizing modeling information from a recently resolved structure of human HIF-1alpha prolyl hydroxylase (EGLN1) and structure-based design, a novel series of imidazo[1,2-a]pyridine derivatives was prepared. The activity of these compounds was determined in a human EGLN1 assay and a limited SAR was developed.
利用来自最近解析的人类低氧诱导因子-1α脯氨酰羟化酶（EGLN1）结构的建模信息以及基于结构的设计，制备了一系列新型咪唑并[1,2-a]吡啶衍生物。在人类EGLN1检测中测定了这些化合物的活性，并建立了有限的构效关系。
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