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

Jie-Fei Cheng,Chi Ching Mak,Yujin Huang,Richard Penuliar,Masahiro Nishimoto,Lin Zhang,Mi Chen,David Wallace,Thomas Arrhenius,Donald Chu,Guang Yang,Miguel Barbosa,Rick Barr,Jason R B Dyck,Gary D Lopaschuk,Alex M Nadzan

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

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.

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关键词

Malonyl-CoA,Acetyl-CoA,Malonyl-CoA decarboxylase,MCD,Fatty acid oxidation,Glucose oxidation

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