Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation

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• 作者：Abhisek Banerjee ; Pravin S. Yadav ; Malini Bajpai ; Ramachandra Rao Sangana ; Srinivas Gullapalli ; Girish S. Gudi ; Laxmikant A. Gharat ; ^{laxmikant_gharat@glenmarkpharma.com}
• 关键词：Phosphodiesterase 7 inhibitors ; Isothiazolopyrimidone ; Isoxazolopyrimidone ; Parkinson&rsquo ; s disease ; CNS penetration
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 May, 2012
• 卷：22
• 期：9
• 页码：3223-3228
• 文件大小：2916 K

摘要

The synthesis and structure-activity relationship studies of isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors are discussed. The pharmacokinetic profile of dFont">10 and dFont">21 with adequate CNS penetration, required for in vivo Parkinson鈥檚 disease models, are disclosed.