Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

A series of substituted 1-hydroxypyrazole analogues of the GABA(A) receptor partial agonist 5-(4-piperidyl)-3-isoxazolol (4-PIOL) have been synthesized and pharmacologically characterized. Several of the analogues displayed K(i) in the low nanomolar range at the native GABA(A) receptors and potent antagonism of the alpha(1)beta(2)gamma(2) receptor. It appears that several regions situated in proximity to the core of the orthosteric binding site of the GABA(A) receptor are able to accommodate large hydrophobic substituents.
TidsskriftJournal of Medicinal Chemistry
Udgave nummer8
Sider (fra-til)3417-3421
StatusUdgivet - 2010

ID: 20197322