Hydroxyazepanes as inhibitors of glycosidase and hiv protease

Details Hydroxyazepanes as inhibitors of glycosidase and hiv protease Hydroxyazepanes as inhibitors of glycosidase and hiv protease

C - Chemistry, Metallurgy

07

D

C07D 223/08 (2006.01) A01N 43/04 (2006.01) C12P 1/00 (2006.01) C12P 13/00 (2006.01) C12P 17/10 (2006.01) C12P 19/00 (2006.01) C12P 19/26 (2006.01)

Patent

CA 2282254

Hydroxyazepanes display inhibitory activity with respect to glycosidase, with K i values from moderate to low micromolar range. Benzyl and 3,6-dibenzyl derivatives of hydroxyazepanes display inhibitory activity with respect to HIV protease. These compounds are synthesized either by chemoenzymatic or chemical methodologies. Methods are provided for producing a tetrahydroxyazepane with the formula: (see formula I)

Les hydroxyazépanes présentent une activité inhibitrice vis-à-vis de la glycosidase, avec des valeurs de micromolarité Ki modérées à faibles. Les dérivés benzyle et 3,6-dibenzyle des hydroxyazépanes présentent une activité inhibitrice vis-à-vis de la VIH-protéase. Ces composés sont synthétisés par des méthodes chimio-enzymatiques ou chimiques.

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