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Biomedical subjects

Sophie Havez

Publications and source records attributed to Sophie Havez.

2 recordsLinked to original sources

Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.

The known KDR inhibitor SU5416 and several analogues of the indolin-2-one family were surprisingly found to be highly efficacious in the EAE model, an established model for multiple sclerosis. The high in vivo effect could be correlated to in vitro inhibition of the pro-inflammatory cytokine IL-2. Activity following po administration was obtained with several analogues and via the use of prodrugs.

Animals↗

Directed ortho-Lithiation on Solid Phase.

Resin-bound 1-hydroxyimidazole, obtained by alkylation of the sodium salt of 1-hydroxyimidazole with chloromethyl polystyrene, was lithiated at C-2 with n-butyllithium. Subsequent treatment with carbon, halogen, or sulfur electrophiles followed by detachment from the solid support by heating with trifluoracetic acid at 100 degrees C for 20 h gave 2-substituted 1-hydroxyimidazoles in 52-93% yields.

Journal Article↗