发现三嗪类化合物是强效、选择性和口服有效的 PDE4 抑制剂。
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
机构信息
BioCrea GmbH, Meissner Strasse 191, 01445 Radebeul, Germany.
出版信息
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4308-14. doi: 10.1016/j.bmcl.2013.05.099. Epub 2013 Jun 10.
PMID:23806553
Abstract
Expanding on HTS hit 4 afforded a series of [1,3,5]triazine derivatives as novel PDE4 inhibitors. The SAR development and optimization process with the emphasis on ligand efficiency and physicochemical properties led to the discovery of compound 44 as a potent, selective and orally active PDE4 inhibitor.
摘要
对高内涵筛选命中物 4 进行扩展得到了一系列[1,3,5]三嗪衍生物，它们是新型 PDE4 抑制剂。以配体效率和物理化学性质为重点的 SAR 开发和优化过程导致发现了化合物 44，它是一种强效、选择性和口服有效的 PDE4 抑制剂。
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