912948-07-3Relevant academic research and scientific papers
NPY ANTAGONISTS, PREPARATION AND USES
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Page/Page column 79, (2009/09/28)
The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
Piperazinyl benzamidines: Synthesis and affinity for the delta opioid receptor
Nortey, Samuel O.,Baxter, Ellen W.,Codd, Ellen E.,Zhang, Sui-Po,Reitz, Allen B.
, p. 1741 - 1743 (2007/10/03)
Piperazinyl benzamidines were prepared and found to bind to the rat delta (δ) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2- (trifluoromethyl)phenyl]iminomethyl]benzamide (27) with a 1.22 nM Ki for the rat δ opioid receptor and ca. 1000× selectivity relative to the μ opioid subtype.
