Title of article
Pyrazoloheteroaryls: Novel p38α MAP kinase inhibiting scaffolds with oral activity
Author/Authors
Laszlo Revesz، نويسنده , , Ernst Blum، نويسنده , , Franco E. Di Padova، نويسنده , , Thomas Buhl، نويسنده , , Roland Feifel، نويسنده , , Hermann Gram، نويسنده , , Peter Hiestand، نويسنده , , Ute Manning، نويسنده , , Ulf Neumann، نويسنده , , Gerard Rucklin، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
262
To page
266
Abstract
A test library with three novel p38α inhibitory scaffolds and a narrow set of substituents was prepared. Appropriate combination of substituent and scaffold generated potent p38α 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.
Keywords
Antiarthritic , anti-inflammatory , adjuvant-induced arthritis , Collagen-induced arthritis , rheumatoid arthritis , MAP kinase inhibition , p38 inhibition
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796355
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