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

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. [Display omitted]...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2016-02, Vol.26 (4), p.1184-1187
Main Authors: Han, Qiang, Pabba, Praveen K., Barbosa, Joseph, Mabon, Ross, Healy, Jason P., Gardyan, Michael W., Terranova, Kristen M., Brommage, Robert, Thompson, Andrea Y., Schmidt, James M., Wilson, Alan G.E., Xu, Xiaolian, Tarver, James E., Carson, Kenneth G.
Format: Article
Language:English
Subjects:
Animals
Benzopyrans - chemistry
Benzopyrans - pharmacokinetics
Benzopyrans - therapeutic use
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacokinetics
Enzyme Inhibitors - therapeutic use
Esterases - antagonists & inhibitors
Esterases - metabolism
Femur - physiology
Femur cortical bone thickness
Half-Life
Humans
Inhibitory Concentration 50
Male
Mice
Notum Pectinacetylesterase
Osteoporosis - drug therapy
Osteoporosis - physiopathology
Osteroporosis
Protein Binding
SAR
Structure-Activity Relationship
Thienochromene
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Summary: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. [Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2016.01.038