发现具有口服活性的吡唑并喹啉作为强效 PDE10 抑制剂，可用于精神分裂症的治疗。
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
出版信息
Bioorg Med Chem Lett. 2012 Jan 1;22(1):235-9. doi: 10.1016/j.bmcl.2011.11.023. Epub 2011 Nov 16.
PMID:22142545
Abstract
A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antipsychotic activity in the MK-801 induced hyperactive rat model.
摘要
已经合成了一系列吡唑并喹啉类似物，并证明它们与 PDE10 具有高亲和力。通过 SAR 研究和我们的先导化合物优化工作，发现化合物 16 和 27 在 MK-801 诱导的多动大鼠模型中具有有效的口服抗精神病活性。
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