Department of Medicinal Chemistry, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):531-6. doi: 10.1016/j.bmcl.2009.11.100. Epub 2009 Nov 24.
An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M(1) positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified.
采用迭代模拟库合成方法探索了一系列选择性 M(1)正变构调节剂的喹诺酮羧酸,确定了提高效力和血浆游离分数的策略。