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The Metabolism of Xylazine in Rats
ParkChoo, Hea-Young,Choi, Sun-Ok The Pharmaceutical Society of Korea 1991 Archives of Pharmacal Research Vol.14 No.4
The biotransformation of xylazine, a widly used animal tranquilizer, was investigated in rats. After administration of xylazine, the existence of 2,6-dimethylphenyl-isothiocyanate, 2,6-dimenthyl-4-hydroxy-aniline and p-hydroxy-xylazine in urine was confirmed by the comparison with chemically prepared standards in GC/MS. The main metabolite, p-hydroxy xylazine was excreted as conjugated form.
3D QSAR Studies on New Piperazine Derivatives with Antihistamine and Antibradykinin Effects
Parkchoo, Hea-Young,Chung, Bum-Jun The Pharmaceutical Society of Korea 2000 Archives of Pharmacal Research Vol.23 No.4
Three dimensional QSAR studies for antihistamine and antibradykinin effects of new piperazine derivatives were conducted using the comparative molecular field analysis. Electrostatic and steric factors, but not hydrophobic factor, of the synthesized compounds were correlated with the antagonistic effect.
Synthesis and Inhibition Effects on 5-HT<sub>6</sub> Receptor of Benzothiazole Derivatives
Hayat, Faisal,Yoo, Euna,Rhim, Hyewhon,ParkChoo, Hea-Young Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-$HT_6$ ligands. In vitro assay was evaluated by measuring the 5-HT-induced $Ca^{2+}$ increases using HeLa cell line expressing the cloned human 5-$HT_6$ receptor, and the compound 13 showed potent 5-$HT_6$ receptor antagonistic effect with $IC_{50}$ value of 3.9 ${\mu}M$. Compound 13 also showed good selectivity on the 5-$HT_6$ over 5-$HT_4$ and 5-$HT_7$ receptors.
Synthesis, Cytotoxicity and Topoisomerase II Inhibitory Activity of Benzonaphthofurandiones
Rhee, Hee-Kyung,Kwon, Young-Joo,Chung, Hwa-Jin,Lee, Sang-Kook,ParkChoo, Hea-Young Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.7
Benzonaphthofurandiones containing four coplanar fused aromatic rings were synthesized and evaluated for their cytotoxicity against five human cancer cell lines, and their inhibitory activity on topoisomerases. These benzonaphthofurandiones were prepared by condensation of 2,3-dichloronaphthoquinone and three aromatic diols with base catalysts in alcohol. The synthesized compounds were o-alkylated with six dialkylaminoalkyl halides. The hydroxy derivatives (8a-8g) exhibited relatively potent cytotoxicity among the prepared compounds. These compounds were evaluated as excellent inhibitors against topoisomerase II (topo II). Especially, the hydroxy analogue with branched methyl side chain (8e) showed high cytotoxicity against cancer cell lines and good inhibitory activity on topo II.
Enantioselective Determination of Cetirizine in Human Urine by HPLC
Choi, Sun-Ok,Lee, Seok-Ho,Kong, Hak-Soo,Kim, Eun-Jung,Parkchoo, Hae-Young The Pharmaceutical Society of Korea 2000 Archives of Pharmacal Research Vol.23 No.2
In order to study the simultaneous determination of (+)- and (-)-cetirizine in human urine we have developed a chiral separation method by HPLC. A chiral stationary phase of $\alpha$$_1$-acidglycoprotein, the AGP-CSP was used to separate the enantiomers. The pH of the phosphate buffer, as well as the content of the organic modifier in the mobile phase, markedly affected the chromatographic separation of (+)- and (-)-cetirizine. A mobile phase of 10 m㏖/1 phosphate buffer (pH 7.0)-acetonitrile (95 : 5, v/v) was used for the urine assays. Ultraviolet absorption was monitored at 230nm and roxatidine was employed as the internal standard for quantification. (+)-Cetirizine, (-)-cetirizine and the internal standard were eluted at retention times of 12, 16, and 32 mins, respectively. The detection limit for cetirizine enantiomers was 400 ng/$m\ell$ of urine. A pharmacokinetic study was conducted with the help of 5 healthy female volunteers who were administered with a single oral dose of racemic cetirizine (20 mg). The peak area ratios provided by the cetirizine enantiomers were linear(r>0.997) over a concentration range of 2.5-200 ${\mu}g/ml$. The peak of the excreted cetirizine enantiomers appeared in the urine sample during the period of 1-2 hrs following the administration of the oral dose. The excreted level of (+)-cetirizine was slightly higher than (-)-cetirizine but the difference was not statistically significant. However, this method appears to have applications for enantioselective pharmacokinetic studies of racemic drugs.
Synthesis of Benzoxazole Amides as Novel Antifungal Agents against Malassezia Furfur
Kim, Beom-Joon,Kim, Jin-Ah,Kim, Young-Kook,Choi, Soon-Yong,ParkChoo, Hea-Young Korean Chemical Society 2010 Bulletin of the Korean Chemical Society Vol.31 No.5
Malassezia is a pathogenic fungus that causes skin diseases, such as tinea versicolor, atopic dermatitis and fatal sepsis. We report the synthesis of a series of benzoxazole amides and evaluation of their antifungal activity against Malassezia furfur. Twelve benzoxazole amides were prepared through the cyclization of the substituted 2-hydroxy aniline with N-(bis-methylsulfanylmethylene) amides. Among the prepared compounds, the compounds 4a, 8b, 8c and 8d showed in vitro antifungal activity.