鉴定甲氧基萘骨架作为喹诺里西啶酮酰胺M(1)正变构调节剂中的核心替代物。
Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.
作者信息
Kuduk Scott D, Di Marco Christina N, Saffold Jonathan R, Ray William J, Ma Lei, Wittmann Marion, Koeplinger Kenneth A, Thompson Charles D, Hartman George D, Bilodeau Mark T, Beshore Douglas C
机构信息
Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2014 Mar 1;24(5):1417-20. doi: 10.1016/j.bmcl.2014.01.012. Epub 2014 Jan 13.
A series of methoxynaphthalene amides were prepared and evaluated as alternatives to quinolizidinone amide M1 positive allosteric modulators. A methoxy group was optimal for M1 activity and addressed key P-gp issues present in the aforementioned quinolizidinone amide series.
制备了一系列甲氧基萘酰胺，并将其作为喹诺里西啶酮酰胺M1正变构调节剂的替代物进行评估。甲氧基对于M1活性是最佳的，并且解决了上述喹诺里西啶酮酰胺系列中存在的关键P-糖蛋白问题。
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