Solid/solution-phase annulation reagents: single-step synthesis of cyclic amine derivatives.
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Amines↗
Biomedical subjects
William Barker
Publications and source records attributed to William Barker.
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
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.
Acetic Acid↗