Revesz, Laszlo, Blum, Ernst, Di Padova, Franco E., Buhl, Thomas, Feifel, Roland, Gram, Hermann, Hiestand, Peter, Manning, Ute, Neumann, Ulf and Rucklin, Gerard (2006) Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity. Bioorganic & Medicinal Chemistry Letters, 16 (2). pp. 262-266. ISSN 0960-894X

Abstract

A test library with three novel p38alpha inhibitory scaffolds and a narrow set of substituents was prepared. Appropriate combination of substituent and scaffold generated potent p38alpha inhibitors, for example, pyrazolo[3,4-b]pyridine 9, pyrazolo[3,4-d]pyrimidine 18a and pyrazolo[3,4-b]pyrazine 23b with potent in vivo activity upon oral administration in animal models of rheumatoid arthritis.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.10.015
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	p38 inhibition; MAP kinase inhibition; Rheumatoid arthritis; Antiarthritic; Anti-inflammatory; Collagen-induced arthritis; Adjuvant-induced arthritis
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.10.015
Date Deposited:	14 Dec 2009 13:59
Last Modified:	31 Jan 2013 01:15
URI:	https://oak.novartis.com/id/eprint/485