4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase

  • Bioorg Med Chem Lett. 2016 Feb 15;26(4):1184-7. doi: 10.1016/j.bmcl.2016.01.038.
Qiang Han  1 ,  Praveen K Pabba  1 ,  Joseph Barbosa  1 ,  Ross Mabon  1 ,  Jason P Healy  1 ,  Michael W Gardyan  1 ,  Kristen M Terranova  1 ,  Robert Brommage  2 ,  Andrea Y Thompson  2 ,  James M Schmidt  2 ,  Alan G E Wilson  2 ,  Xiaolian Xu  1 ,  James E Tarver Jr  3 ,  Kenneth G Carson  1
Affiliations
  • 1. Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • 2. Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
  • 3. Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States. Electronic address: [email protected].
PMID: 26821819 DOI: 10.1016/j.bmcl.2016.01.038
Abstract

A group of small molecule thienochromenes inhibitors of Notum Pectinacetylesterase are described. We developed SAR on three series based on carbon, oxygen and sulfur replacement of the 5-position. In each series, highly potent Notum Pectinacetylesterase inhibitors were identified.

Keywords
Femur cortical bone thickness; Notum Pectinacetylesterase; Osteroporosis; SAR; Thienochromene.
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