鉴定哒嗪并[4,5-b]吲唑啉类化合物为选择性 PDE4B 抑制剂。
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors.
机构信息
Worldwide Medicinal Chemistry, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2163-7. doi: 10.1016/j.bmcl.2010.02.044. Epub 2010 Feb 13.
PMID:20202838
Abstract
Substituted pyridazino[4,5-b]indolizines were identified as potent and selective PDE4B inhibitors. We describe the structure-activity relationships generated around an HTS hit that led to a series of compounds with low nanomolar affinity for PDE4B and high selectivity over the PDE4D subtype.
摘要
取代的吡啶并[4,5-b]吲唑被鉴定为强效和选择性 PDE4B 抑制剂。我们描述了围绕高通量筛选命中化合物生成的构效关系，这些化合物对 PDE4B 具有低纳摩尔亲和力和对 PDE4D 亚型的高选择性。
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