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三取代和四取代咪唑作为 p38α 丝裂原活化蛋白激酶抑制剂。

Tri- and tetrasubstituted imidazoles as p38α mitogen-activated protein kinase inhibitors.

机构信息

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Eberhard Karls University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.

出版信息

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6671-5. doi: 10.1016/j.bmcl.2010.09.012. Epub 2010 Sep 9.

DOI:10.1016/j.bmcl.2010.09.012
PMID:20934337
Abstract

The synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles as potent p38α mitogen-activated protein kinase inhibitors is described. The trisubstituted imidazole series was found to be more potent than the tetrasubstituted imidazole series. Many of these compounds show low-nanomolar activities in the isolated p38α MAP kinase inhibition assay. The structure-activity relationships between these two series are different and not comparable.

摘要

描述了作为强效 p38α 有丝分裂原激活的蛋白激酶抑制剂的 2,4,5-三取代和 1,2,4,5-四取代咪唑的合成。三取代咪唑系列比四取代咪唑系列更有效。这些化合物中的许多在分离的 p38α MAP 激酶抑制测定中显示出低纳摩尔的活性。这两个系列之间的构效关系不同，不可比较。

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