Kyoung Hee Byoun

Synthesis and structure-activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-α.

3-Alkyl-2-aryl-2-cyclopenten-1-one oxime derivatives (1) were studied as a novel class of inhibitors of tumor necrosis factor α (TNF-α) with regard to synthesis and in vitro SAR inhibition of TNF-α. The in vitro IC50 values of these compounds in rat and human peripheral blood mononuclear cells were at the sub-micromolar level.

Whitening Effects of Adamantyl Benzamide Derivatives

The structure activity relationship of polyhydroxylated benzamide derivatives for whitening effects was examined. The adamantyl benzamide derivatives with catechol (3,4-dihydroxyphenyl) of B-ring part showed good anti-melanogenesis activity, but the inhibitory activity of mono-hydroxyphenyl (3-OH or 4-OH) or 3,4-dimethoxyphenyl substituted derivatives was decreased or lost. Therefore the catechol unit was appeared to be the crucial factor for the inhibition of melanogenesis. And the existence of 2-OH of A-ring part had minor influence on the activity, the length of carbon chain between A-ring and B-ring was also not the major factor for the anti-melanogenesis activity.

Improved One-pot Regioselective Synthesis of 3,7-Diarylpyrazolo[1,5-α]pyrimidines and Their CB1R Activity

This study demonstrates an effective one-pot regioselective synthesis of 3,7-diarylpyrazolo [1,5-α]pyrimidines. Moreover, the derivatives obtained were effective CB1R antagonists. These pyrazolo [1,5-α]pyrimidines with diaryl groups at the 3,7-positions are potential pharmacophores for CB1R candidates.