30684-07-2Relevant academic research and scientific papers
Transformation of Monoamine Oxidase-B Primary Amine Substrates into Time-Dependent Inhibitors. Tertiary Amine Homologues of Primary AMine Substrates
Ding, Charles Z.,Lu, Xingliang,Nishimura, Kuniko,Silverman, Richard B.
, p. 1711 - 1715 (2007/10/02)
A family of N-methylated and N,N-dimethylated alkyl and arylalkylamines was prepared and more than half of the analogues were shown to be time-dependent pseudo-first-order inhibitors of monoamine oxidase-B.Some of the time-dependent inactivators were reversible and others were irreversible with respect to prolonged dialysis following inactivation.Partition ratios ranged from zero to 11 000.These results are rationalized in terms of a combination of an inductive effect and a stereoelectronic effect as a result of hindered rotation of an active site covalent adduct.A molecualr mechanics calculation indicates that there is at least 10 kcal/mol of torsional energy to be overcome in order for the enzyme adduct to be released.These findings show that tertiary amine homologues of primary amine substrates of monoamino oxidase are time-dependent inhibitors, and this should be useful in the design of new inactivators of this enzyme.
Polycyclic amines and intermediates therefor
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, (2008/06/13)
This invention relates to a new method for the preparation of amines containing alkylene groups by using cyclic alkylene sulphuric esters, and novel intermediates for use in the method. The new method is useful for preparation of i.a. pharmaceuticals. The novel intermediates are useful i.a. as surfactants.
