| Literature DB >> 15482950 |
Paul A Tuthill1, Pamela R Seida, William Barker, Joel A Cassel, Serge Belanger, Robert N DeHaven, Michael Koblish, Susan L Gottshall, Patrick J Little, Diane L DeHaven-Hudkins, Roland E Dolle.
Abstract
A new class of kappa-opioid receptor agonists is described. The design of these agents was based upon energy minimization and structural overlay studies of the generic azepin-2-one structure 3 with the crystal structure of arylacetamide kappa agonist 1, ICI 199441. The most active compound identified was ligand 4a (K(i)=0.34 nM), which demonstrated potent antinociceptive activity after oral administration in rodents.Entities:
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Year: 2004 PMID： 15482950 DOI： 10.1016/j.bmcl.2004.08.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823