The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents
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DOI：
10.1016/j.bmcl.2009.03.024
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发表时间：
2009-05-01
影响因子：
2.7
通讯作者：
Gibbs, E. Michael
中科院分区：
文献类型：
--
作者：
DeNinno, Michael P.;Andrews, Melissa;Gibbs, E. Michael
从非选择性吡唑并嘧啶酮先导化合物开始，平行药物化学的连续使用和定向合成导致了有效、高选择性和口服生物可利用的 PDE9 抑制剂的发现。这些工具的可用性允许对 PDE9 抑制的治疗潜力进行全面评估。 (C) 2009 Elsevier Ltd. 保留所有权利。
Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of PDE9 inhibition. (C) 2009 Elsevier Ltd. All rights reserved.