N-Acylhydrazones as inhibitors of PDE10A

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• 作者：Jennifer L. Gage^a ; Rene Onrust^a ; Derek Johnston^b ; Andrew Osnowski^b ; Wendy MacDonald^b ; Lee Mitchell^b ; L&#xe1 ; szl&#xf3 ; Ü ; r&#xf6 ; gdi^c ; Alex Rohde^a ; Kevin Harbol^a ; Sasha Gragerov^a ; Gy&#xf6 ; rgy Dorm&#xe1 ; n^c ; Tom Wheeler^a ; Vince Florio^a ; Neil S. Cutshall^a ; ^{ncutshall@omeros.com"" rel=""nofollow}
• 关键词：PDE10 ; PDE10A ; Phosphodiesterase ; Schizophrenia ; Hydrazide ; PDE ; Enzyme inhibitor ; Hydrazone ; Acylhydrazone
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 July 2011
• 年：2011
• 卷：21
• 期：14
• 页码：4155-4159
• 全文大小：1247 K

文摘

Cyclic nucleotide phosphodiesterases (PDEs) are represented by a large superfamily of enzymes. A series of hydrazone-based inhibitors was synthesized and shown to be novel, potent, and selective against PDE10A. Optimized compounds of this class were efficacious in animal models of schizophrenia and may be useful for the treatment of this disease.