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

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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.