N-杂环衍生的 M1 正变构调节剂。
N-heterocyclic derived M1 positive allosteric modulators.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1334-7. doi: 10.1016/j.bmcl.2010.01.013. Epub 2010 Jan 11.
PMID:20097564
Abstract
Replacement of a phenyl ring with N-linked heterocycles in a series of quinolone carboxylic acid M1 positive allosteric modulators was investigated. In particular, a pyrazole derivative exhibited improvements in potency, free fraction, and CNS exposure.
摘要
研究了一系列喹诺酮羧酸 M1 正变构调节剂中 N 连接杂环取代苯环。特别是，吡唑衍生物在效力、游离分数和中枢神经系统暴露方面得到了改善。
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