• Archives of Pharmacal Research
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• v.21 no.4
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• pp.440-444
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• 1998

A series of 6-(N-arylamino)-7-methylthio-5,8-quinolinedione derivatives 4a-4l was newly synthesized for the evaluation of antifungal activity. 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones were prepared by regioselective nucleophilic substitution of 6,7-dichloro-5,8-quinolinediones with arylamines in the presence of $Ce^{3+}$, and $Na_2$S/dimethylsulfate. The MIC values of 4a-4l were determined for antifungal susceptibility in vitro against Candida species by agar streak method. The derivatives 4a-4l had generally potent antifungal activities against all human pathogenic fungi. Especially they had the most potent activity against C. krusei at 12.5-0.8 $\mu\textrm{g}$/ml. Compounds 4d, 4g, 4h, 4j and 4k had more potent antifungal activities than fluconazole. Compounds 4g and 4h completely inhibited the fungal growth at 0.8-6.3 $\mu\textrm{g}$/ml against all Candida species, while fluconazole inhibited the growth at 25 $\mu\textrm{g}$/ml. The compounds such as 4g and 4h containing an N-(4-bromo-2-methylphenyl)- or N-(4-bromo-3methylphenyl)amino substituent exhibited the most potent antifungal activities.

• Nuclear Engineering and Technology
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• v.37 no.4
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• pp.391-394
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• 2005

N-(3-bromo-2,4,6-trimethylacetanilide)iminodiacetic acid (BrTIDA) was synthesized using nitrilotriacetic anhydride prepared in situ, and lyophilized vials were prepared which contained 20 mg of BrTIDA and 0.4 mg of $SnCl_2$. To evaluate the clinical efficacy of the in-house prepared lyophilized kit, a technetium-99m complex of BrTIDA was prepared; its in vivo pharmacokinetic behavior was evaluated via animal studies to assess the hepatocytic function and the functional status of the cystic duct and the gallbladder. Serial static image scans of rabbits and the biodistribution in mice injected with $^{99m}Tc-BrTIDA$ revealed that none of the tissues except for the hepatobiliary system showed radioactivity concentrations, and a rapid clearance from the organs was observed. In conclusion, a lyophilized kit and its prepared $^{99m}Tc-BrTIDA$ can be applied as a hepatobiliary imaging agent for the evaluation of the functional status of the hepatocytes and the patency of the biliary duct.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.3
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• pp.227-237
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• 2021

Carbon monoxide (CO) is a cardioprotectant and potential cardiovascular therapeutic agent. Human cardiac fibroblasts (HCFs) are important determinants of myocardial structure and function. Large-conductance Ca2+-activated K+ (BK) channel is a potential therapeutic target for cardiovascular disease. We investigated whether CO modulates BK channels and the signaling pathways in HCFs using whole-cell mode patch-clamp recordings. CO-releasing molecules (CORMs; CORM-2 and CORM-3) significantly increased the amplitudes of BK currents (IBK). The CO-induced stimulating effects on IBK were blocked by pre-treatment with specific nitric oxide synthase (NOS) blockers (L-NG-monomethyl arginine citrate and L-NG-nitroarginine methyl ester). 8-bromo-cyclic GMP increased IBK. KT5823 (inhibits PKG) or ODQ (inhibits soluble guanylate cyclase) blocked the CO-stimulating effect on IBK. Moreover, 8-bromo-cyclic AMP also increased IBK, and pre-treatment with KT5720 (inhibits PKA) or SQ22536 (inhibits adenylate cyclase) blocked the CO effect. Pre-treatment with N-ethylmaleimide (a thiol-alkylating reagent) also blocked the CO effect on IBK, and DL-dithiothreitol (a reducing agent) reversed the CO effect. These data suggest that CO activates IBK through NO via the NOS and through the PKG, PKA, and S-nitrosylation pathways.

• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1741-1744
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• 2011

• YAKHAK HOEJI
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• v.46 no.6
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• pp.375-380
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• 2002

In this study, newly designed COX-2 inhibitors, synthetic derivatives of benzothiazine-3-carboxamide, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. 7-Bromo-1,2-benzoisothiazine derivatives were obtained from 4-bromotoluene over the chlorosulfonation, amination and oxidation. And benzothiazine ring was synthesized through Gabriel-Colmann rearrangement reaction. To evaluate inhibitory effect of COX-2, synthetic derivatives of benzothiazine-3-carboxamide were tested with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Some of the synthesized lead compounds have potentially shown the structure-activity relationship for selectivity of COX-2 inhibition activity.

• YAKHAK HOEJI
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• v.17 no.1
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• pp.17-20
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• 1973

Six novel compounds of N,N-dimethyl-N'-(6-substituted-2-benzothiazolyl) formamidines nad six novel compounds of N, N-dimethyl-N'-(substituted-phenyl)formamidines were synthesized. They were evaluated fro their bactericidal activities aginst Salmonella typhoso, Escherichia coli, Vibrio cholera, Staphyloccus aureus, Sarcina lutea and for their fungicidal activities against Saccharomyces cereviseae, Candida albicans. It was found that these compounds were considerably more active than phenol, especially against Vibrio cholera, and N, N-dimethy-N'-(4-methyl-phenyl_formamkidine, N, N-dimethyl-N'-(2-methyl-4-bromo-phenyl)formanidine showed most potent bactericidal activities.

• Bulletin of the Korean Chemical Society
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• v.23 no.11
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• pp.1611-1615
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• 2002

The ring opening of epoxides with elemental iodine and bromine in the presence of three diamine podands 7-9 as new catalysts affords vicinal iodo alcohols and bromo alcohols in high yields. This new procedure occurs regioselectively under neutral and mild conditions in various aprotic solvents even when sensitive functional groups are presented.

• Bulletin of the Korean Chemical Society
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• v.23 no.9
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• pp.1272-1287
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• 2002

Sonochemical Reformatsky reaction of aldehydes or ketones with ethyl bromoacetate in the presence of indium afforded $\beta-hydroxyesters$ in good to excellent yields under mild conditions. 2- or 3-Hydroxybenzaldehyde that contains an acidic hydrogen r eacted with ethyl bromoacetate to provide the desired compounds with the same efficiency. In the case of ethyl 2-bromopropanoate and ethyl 2-bromo-2-methylpropanoate, the desired products were obtained in good yields. Reaction of aldehyde with indium reagent in the presence of ketone group proceeded chemoselectively.

• Toxicological Research
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• v.34 no.1
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• pp.83-83
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• 2018

• Journal of Photoscience
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• v.12 no.2
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• pp.83-85
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• 2005

Photochemical reactivities of ${\beta}-ethoxypropiophenones$ are changed dramatically by putting a halogen at a position to the carbonyl functionality. ${\alpha}-Bromo-{\beta}-ethoxypropiophenone$ gives C-Br bond cleavage products solely, but ${\alpha}-chloro-{\beta}-ethoxypropiophenone$ forms mainly the Yang photocyclization products upon irradiation. The different reactivities of two compounds can be explained by relative rates of C-X bond cleavage and a-hydrogen abstraction.