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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-02, Vol.26 (4), p.1184-1187
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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