An optimized strategy for the synthesis of the potent p38α mitogen-activated protein kinase inhibitors 2-(2-hydroxyethylsulfanyl)-4-(4-fluorophenyl)-5-(2-aminopyridin-4-yl)imidazole (3) and 2-(2,3-dihydroxypropylsulfanyl)-4-(4-fluorophenyl)-5-(2-aminopyridin-4-yl)imidazole (4) starting from 2-fluoro-4-methylpyridine is reported. In contrast to a previously published synthesis starting from 2-br...

A series of 2-alkylsulfanyl-4-(4-fluorophenyl)-5-(2-aminopyridin-4-yl)-substituted imidazoles was prepared and interaction possibilities of the 2-thioether moiety with phosphate/ribose binding pockets of p38 MAP kinase were investigated. Introduction of the alkyl/benzyl amino function at the pyridine moiety was carried out via nucleophilic substitution or via palladium catalyzed aryl-C-N-bond f...

A novel series of N-(3-(6-substituted-aminopyridin-3-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting TrkA receptor tyrosine kinase was identified. SAR study of the series allowed us to design and synthesize compounds possessing inhibitory activity of TrkA kinase enzyme in the low nanomolar range with low residual activity against c-Met and with no significant activity against...

On the basis of biologically active 3-aminopyridine-2(1H)-ones, authors carried out chemical modification into derivatives corresponding monothiooxamides for first time. It has been shown that 3-aminopyridin-2(1H)-oneenter transamidation reactions with hydrazine-hydrate and are further cyclized under action chloroacetyl chloride conjugated 1,3,4-thiadizole derivatives.

this work described an efficient pseudo four-component synthesis of (10e)-n-benzylidene-2-phenylh-imidazo[1,2-a]pyridin-3-amine derivatives from 2-aminopyridin, malononitrile and arylaldehydes in the presence of naoh under solvent-free and conventional heating condition in good to excellent yields. a wide range of aromatic aldehydes would easily undergo condensations with 2-aminopyridin and mal...

This work described an efficient Pseudo four-component synthesis of (10E)-N-benzylidene-2-phenylH-imidazo[1,2-a]pyridin-3-amine derivatives from 2-aminopyridin, malononitrile and arylaldehydes in the presence of NaOH under solvent-free and conventional heating condition in good to excellent yields. A wide range of aromatic aldehydes would easily undergo condensations with 2-aminopyridin and mal...