Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase

使用噻吩并嘧啶类 Notum 果胶乙酰酯酶抑制剂刺激皮质骨形成

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作者:James E Tarver Jr, Praveen K Pabba, Joseph Barbosa, Qiang Han, Michael W Gardyan, Robert Brommage, Andrea Y Thompson, James M Schmidt, Alan G E Wilson, Wei He, Victoria K Lombardo, Kenneth G Carson

Abstract

A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.

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