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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2004.03.006
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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2004.03.006
Date Deposited:	14 Dec 2009 13:54
Last Modified:	31 Jan 2013 01:07
URI:	https://oak.novartis.com/id/eprint/761