Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.
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Ullrich, Thomas, Baumann, Karl, Welzenbach, Karl, Schmutz, Simone, Camenisch, Gian P., Meingassner, Josef and Weitz Schmidt, Gabriele (2004) Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain. Bioorganic & Medicinal Chemistry Letters, 14 (10). pp. 2483-2487. ISSN 0960-894X
Abstract
Modification of the vanillyl substituent on a potent, semisynthetic lymphocyte function-associated antigen (LFA)-1/intercellular adhesion molecule (ICAM)-1 binding inhibitor of the statin family resulted in metabolically more stable analogues that displayed submicromolar inhibitory activity in vitro and considerable anti-inflammatory activity in vivo. The benzodioxole derivative 2b emerged with the best overall profile.
| Item Type: | Article |
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| Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Statins; LFA-1 inhibitors; Allergic contact dermatitis; Microsomal stability |
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| Date Deposited: | 14 Dec 2009 13:54 |
| Last Modified: | 31 Jan 2013 01:07 |
| URI: | https://oak.novartis.com/id/eprint/761 |