Bioorganic & Medicinal Chemistry Letters 2018-04-07

Agonists of the γ-Aminobutyric Acid Type B (GABAB) Receptor Derived from β-Hydroxy and β-Amino Difluoromethyl Ketones

Munia F. Sowaileh, Amy E. Salyer, Kuldeep K. Roy, Jinu P. John, James R. Woods, Robert J. Doerksen, Gregory H. Hockerman, David A. Colby

Index: 10.1016/j.bmcl.2018.04.003

Full Text: HTML

Abstract

Highlights • β-Hydroxy difluoromethyl ketones have distinct SAR data at the GABAB receptor. • β-Amino difluoromethyl ketones are now characterized as GABAB agonists. • Docking studies at the GABAB receptor suggest similar binding modes to baclofen.

Latest Articles:

Design, synthesis, evaluation, and molecular docking of ursolic acid derivatives containing a nitrogen heterocycle as anti-inflammatory agents

2018-04-11

[10.1016/j.bmcl.2018.04.021]

Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ

2018-04-10

[10.1016/j.bmcl.2018.04.017]

Valproic Acid Induces Three Novel Cytotoxic Secondary Metabolites in Diaporthe sp., an Endophytic Fungus from Datura inoxia Mill

2018-04-10

[10.1016/j.bmcl.2018.04.018]

Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine D3 receptor ligands with extended functionality for probing the secondary binding pocket

2018-04-04

[10.1016/j.bmcl.2018.03.084]

Structure-Activity Relationship Study of a Series of Caspase Inhibitors Containing γ-Amino Acid Moiety for Treatment of Cholestatic Liver Disease

2018-04-04

[10.1016/j.bmcl.2018.04.002]

More Articles...