Kuduk Scott D, Di Marco Christina N, Chang Ronald K, Ray William J, Ma Lei, Wittmann Marion, Seager Matthew A, Koeplinger Kenneth A, Thompson Charles D, Hartman George D, Bilodeau Mark T
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2533-7. doi: 10.1016/j.bmcl.2010.02.096. Epub 2010 Mar 3.
The phenyl ring in a series of quinolone carboxylic acid M(1) positive allosteric modulators was replaced with a variety of heterocycles in order to reduce protein plasma binding and enhance CNS exposure.
为了降低蛋白质血浆结合率并提高中枢神经系统暴露率,在一系列喹诺酮羧酸M(1)正变构调节剂中,苯环被多种杂环所取代。