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Substituted Isoxazoles as Potent Inhibitors of p38 MAP Kinase

✍ Scribed by Stefan A. Laufer; Simona Margutti; Martina D. Fritz

Publisher: John Wiley and Sons
Year: 2006
Tongue: English
Weight: 205 KB
Volume: 1
Category: Article
ISSN: 1860-7179
DOI: 10.1002/cmdc.200500025

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✦ Synopsis

Abstract

In a continuous effort to develop improved p38 MAP (mitogen‐activated protein) kinase inhibitors, we focused our attention on the suitability of the isoxazole ring as a bioisosteric replacement for the imidazole ring of SB‐203580. 3,4‐ and 4,5‐disubstituted as well as 3,4,5‐trisubstituted isoxazole derivatives were synthesized. These compounds were tested in an in vitro enzyme‐linked immunosorbent assay of isolated p38 MAP kinase and for inhibitory potency against cytochrome P450. Compound 4 a displays a highly promising profile for development as an anti‐inflammatory agent owing to its enhanced suppression of cytokine release, decreased affinity for cytochrome P450 and a twofold decrease in IC~50~ toward isolated p38 MAP kinase.

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