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

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

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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