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Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.

Revesz, Laszlo and Blum, Ernst and Di Padova, Franco E. and Buhl, Thomas and Feifel, Roland and Gram, Hermann and Hiestand, Peter and Manning, Ute and 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
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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
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Date Deposited: 14 Dec 2009 13:59
Last Modified: 31 Jan 2013 01:15
URI: https://oak.novartis.com/id/eprint/485

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