1046494-85-2Relevant articles and documents
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor
Del Giudice, Maria Rosaria,Borioni, Anna,Bastanzio, Giuditta,Sbraccia, Maria,Mustazza, Carlo,Sestili, Isabella
experimental part, p. 1207 - 1221 (2011/04/23)
Bivalent ligands constituted by two identical pharmacophores structurally related to the Nociceptin Opioid Receptor (NOPr) antagonist JTC-801 were synthesized and their binding affinities for NOPr were evaluated. The novel ligands are formed by two modifi
Dibenzoxepinone hydroxylamines and hydroxamic acids: Dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity
Hamer, R. Richard L.,Tegeler, John J.,Kurtz, Ellen S.,Allen, Richard C.,Bailey, Steven C.,Elliott, Mary Ellen,Hellyer, Luther,Helsley, Grover C.,Przekop, Penelope,Freed, Brian S.,White, John,Martin, Lawrence L.
, p. 246 - 252 (2007/10/03)
Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5- lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the arachidonic acid-induced murine ear edema model. On the basis of their promising profile of in vitro and in vivo activities, hydroxamic acids 24h, 3-(6,11-dihydro-11-oxodibenz[b,e]oxepin-2-yl)-N-hydroxy-N-methylpropanamide (HP 977), and 25, 3-(6,11-dihydrodibenz[b,e]oxepin-2-yl)-N-hydroxy-N- methylpropanamide (P10294), were selected as developmental candidates for the topical treatment of inflammatory skin disorders.