Jae Gyu Park

Synthesis and biological activity of annulated pyrazoles as selective COX-2 inhibitors. I.

A series of disubstituted 4,5-polymethylenepyrazoles were synthesized and evaluated their inhibitory activities against COX-2. Some compounds showed strong (0.3nM) inhibitory activity on COX-2 and were found somewhat selective (up to 16) on COX-2 over COX-1.

Synthesis and biological activity of conformationally controlled 2-PAM derivatives

A series of conformationally controlled 2-PAM derivatives were prepared from 2-acetylpyridine and 2,3-pyrido[b]cycloalkenones in two steps and their reactivities towards parathion poisoned AChE were evaluated. The most planar 2,3-pyrido[b]cyclohexanone oxime methiodide showed an activity comparable to 2-PAM implying E-syn is that the most active comformation of 2-PAM in the biological system.

Synthesis and properties of 3,2′-polymethylene-6-(2″-pyridyl)-2-phenylpyridines and their cycloplatinated complexes

Abstract A series of 3,2′-polymethylene bridged 6-(2′-pyridyl)-2-phenylpyridines was prepared from benzo-fused cycloalkanone and β-(dimethyl-amino) vinyl 2-pyridyl ketone as potential N , N , C -terdentates. Preparations and properties of their cycloplatinated complexes were described. Even highly distorted 3,2′-tetramethylene-6-(2″-pyridyl)-2-phenylpyridine can undergo cycloplatination.

Analysis of metabolomic profile of fermented Orostachys japonicus A. Berger by capillary electrophoresis time of flight mass spectrometry

Microbial cell performance in food biotechnological processes has become an important concern for improving human health worldwide. Lactobacillus plantarum, which is widely distributed in nature, is a lactic acid bacterium with many industrial applications for fermented foods or functional foods (e.g., probiotics). In the present study, using capillary electrophoresis time of flight mass spectrometry, the metabolomic profile of dried Orostachys japonicus A. Berger, a perennial medicinal herb with L. plantarum was compared with that of O. japonicus fermented with L. plantarum to elucidate the metabolomic changes induced by the fermentation process. The levels of several metabolites were changed by the fermentation process, indicating their involvement in microbial performance. For example, glycolysis, the pentose phosphate pathway, the TCA cycle, the urea cycle-related metabolism, nucleotide metabolism, and lipid and amino acid metabolism were altered significantly by the fermentation process. Although the fermented metabolites were not tested using in vivo studies to increase human health benefits, our findings provide an insight into the alteration of metabolites induced by fermentation, and indicated that the metabolomic analysis for the process should be accompanied by fermenting strains and conditions.

Design, synthesis and anticonvulsive activities of potential prodrugs linked by two-carbon chain

For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, γ-aminobutyric acid (GABA), γ-vinyl GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential prodrugs and evaluated for their anticonvulsive activities.