Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors

A series of heteroaryl-substituted bis-trifluoromethyl carbinols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some thiazole-based derivatives showed potent in vitro MCD inhibitory activities and significantly increased glucose oxidation rates in isolated working rat hearts.

A series of heteroaryl-substituted bis-trifluoromethyl carbinols 3 were prepared and evaluated as malonyl-CoA decarboxylase inhibitors. Several thiazole derivatives showed potent in vitro inhibitory activities and caused a 5-fold stimulation of glucose oxidation rates in isolated working rat hearts.Figure optionsDownload as PowerPoint slide