当前位置：
X-MOL 学术
›
J. Med. Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A Wingless β-Catenin Agonist That Increases Bone Formation Rate
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2009-10-26 00:00:00 , DOI: 10.1021/jm9014197 Jeffrey C Pelletier 1 , Joseph T Lundquist , Adam M Gilbert , Nipa Alon , Frederick J Bex , Bheem M Bhat , Mattew G Bursavich , Valerie E Coleburn , Luciana A Felix , Daniel M Green , Paula Green , Diane B Hauze , Yogendra P Kharode , Ho-Sun Lam , Susan R Lockhead , Ronald L Magolda , Jeanne J Matteo , John F Mehlmann , Colleen Milligan , Richard J Murrills , Jennifer Pirrello , Sally Selim , Michael C Sharp , Ray J Unwalla , Matthew D Vera , Jay E Wrobel , Paul Yaworsky , Peter V N Bodine
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2009-10-26 00:00:00 , DOI: 10.1021/jm9014197 Jeffrey C Pelletier 1 , Joseph T Lundquist , Adam M Gilbert , Nipa Alon , Frederick J Bex , Bheem M Bhat , Mattew G Bursavich , Valerie E Coleburn , Luciana A Felix , Daniel M Green , Paula Green , Diane B Hauze , Yogendra P Kharode , Ho-Sun Lam , Susan R Lockhead , Ronald L Magolda , Jeanne J Matteo , John F Mehlmann , Colleen Milligan , Richard J Murrills , Jennifer Pirrello , Sally Selim , Michael C Sharp , Ray J Unwalla , Matthew D Vera , Jay E Wrobel , Paul Yaworsky , Peter V N Bodine
Affiliation
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt β-catenin cellular messaging system. Hit-to-lead in vitro optimization for target activity and molecular properties led to the discovery of (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine (5, WAY-262611). Compound 5 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration.
中文翻译：
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine：一种无翼β-连环蛋白激动剂，可提高骨形成率
一项旨在发现治疗骨疾病的小分子先导药物的高通量筛选活动以发现一种具有 2-氨基嘧啶模板的化合物而结束，该模板靶向 Wnt β-连环蛋白细胞信息系统。Hit-to-lead 体外优化靶点活性和分子特性导致发现 (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine ( 5 , WAY- 262611）。化合物5具有优异的药代动力学特性，并且在口服给药后卵巢切除大鼠的骨小梁形成率显示出剂量依赖性增加。
更新日期：2009-10-26
中文翻译：
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine：一种无翼β-连环蛋白激动剂，可提高骨形成率
一项旨在发现治疗骨疾病的小分子先导药物的高通量筛选活动以发现一种具有 2-氨基嘧啶模板的化合物而结束，该模板靶向 Wnt β-连环蛋白细胞信息系统。Hit-to-lead 体外优化靶点活性和分子特性导致发现 (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine ( 5 , WAY- 262611）。化合物5具有优异的药代动力学特性，并且在口服给药后卵巢切除大鼠的骨小梁形成率显示出剂量依赖性增加。
京公网安备 11010802027423号