Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase. Issue 6 (15th March 2016)

• Record Type: Journal Article
• Authors: Tarver, James E.; Pabba, Praveen K.; Barbosa, Joseph; Han, Qiang; Gardyan, Michael W.; Brommage, Robert; Thompson, Andrea Y.; Schmidt, James M.; Wilson, Alan G.E.; He, Wei; Lombardo, Victoria K.; Carson, Kenneth G.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 6(2016)
• Page Start: 1525
• Page End: 1528
• Publication Date: 2016-03-15
• Subjects: Notum Pectinacetylesterase -- Osteoporosis -- Thienopyrimidine -- SAR -- Femur cortical bone thickness; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.02.021
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical 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. 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.