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 10 and 21 with adequate CNS penetration, required for in vivo Parkinson鈥檚 disease models, are disclosed.