15501-39-0Relevant articles and documents
N-heterocyclic inhibitors of TNF-α expression
-
, (2008/06/13)
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
N-heterocyclic inhibitors of TNF-alpha expression
-
, (2008/06/13)
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
Hydrolysis of Unsymmetrical Acetamidines: Leaving Abilities and Stereoelectronic Effects
Perrin, Charles L.,Nunez, Oswaldo
, p. 522 - 527 (2007/10/02)
Unsymmetrical acetamidines hydrolyze in alkaline D2O to a mixture of two acetamides and two amines.Product ratios from three N-methylated acetamidines and five N-alkyl-N'-methylacetamidines were determined by NMR.The direction of cleavage is determined largely by the relative basicities of the two amines, rather than by the relative basicities of the two nitrogens in the tetrahedral intermediate.Steric repulsion in the product amides can also affect the product ratio, but only slightly.There is also a novel configurational effect, which favors cleavage of the nitrogen whose alkyl group is (Z) in the amidinium ion.This arises from a stereoelectronic preference for cleavage of a leaving group that is antiperiplanar to two lone pairs in the tetrahedral intermediate.However, it is concluded that this preference is weak.These results have guided the design of a test of this stereoelectronic preference in the hydrolysis of a set of cyclic amidinium ions where product stabilities and leaving abilities can be closely matched.