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Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.

Ullrich, Thomas and Baumann, Karl and Welzenbach, Karl and Schmutz, Simone and Camenisch, Gian P. and 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

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