4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 6, Pages 1525-1528

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.02.021

Keywords

Notum Pectinacetylesterase; Osteoporosis; Thienopyrimidine; SAR; Femur cortical bone thickness

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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. (C) 2016 Elsevier Ltd. All rights reserved.

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