From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors

From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors

In vitro and in vivo metabolism studies revealed that 2-alkylsulfanylimidazole ML3403 (4-(5-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-4-yl)-N-(1-phenylethyl)pyridin-2-amine) undergoes rapid oxidation to the sulfoxide. Replacing the sulfur atom present in the two potent p38α mitogen-activated prote...

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Bibliographic Details
Main Authors: Fabian Heider, Urs Haun, Eva Döring, Mark Kudolo, Catharina Sessler, Wolfgang Albrecht, Stefan Laufer, Pierre Koch
Format: Article
Language:English
Published: MDPI AG 2017-10-01
Series:Molecules
Subjects:
kinase inhibitors
p38α MAP kinase
trisubstituted imidazoles
metabolic stability
Alzheimer’s disease
neurodegenerative diseases
cancer
Online Access:https://www.mdpi.com/1420-3049/22/10/1729

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