利用前瞻性设计和化学强化策略鉴定一种脑穿透 PDE9A 抑制剂作为快速先导优化策略。
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
机构信息
Neuroscience Chemistry, Pfizer Global Research and Development, Groton, CT 06340, USA.
出版信息
J Med Chem. 2009 Dec 24;52(24):7946-9. doi: 10.1021/jm9015334.
PMID:19919087
Abstract
By use of chemical enablement and prospective design, a novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP.
摘要
通过化学激活和前瞻性设计，我们鉴定了一系列新型的、可穿透血脑屏障的选择性 PDE9A 抑制剂，这些抑制剂能够在体内引起脑 cGMP 的升高。
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