(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors
A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3- ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
Bamford, Mark J.,Alberti, Michael J.,Bailey, Nicholas,Davies, Susannah,Dean, David K.,Gaiba, Alessandra,Garland, Stephen,Harling, John D.,Jung, David K.,Panchal, Terence A.,Parr, Christopher A.,Steadman, Jon G.,Takle, Andrew K.,Townsend, James T.,Wilson, David M.,Witherington, Jason
p. 3402 - 3406
(2007/10/03)
The ortho effect in pyridines. Part XI(1). Substituent effects on basicity of 2- and 4-substituted 3-aminopyridines
The substituent effects on the pKa values corresponding to the first protonation site of thirty 2- and 4-substituted 3-aminopyridines have been studied.It was found that the relative localized and delocalized effects are apparently sensitive to the variation of substituent position in the pyridine ring.An interaction of the 2-substituent with the protonation centre has mainly inductive character, whereas, the pKa values of 4-substituted 3-aminopyridines are highly affected by through-resonance.The steric effect was found to be insignificant.Keywords: substituent effects / 2- and 4-substituted 3-aminopyridines / basicity
Rasala, D.
p. 79 - 84
(2007/10/02)
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