• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.342.1-342.1
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• 2002

6.7-Dicholroquinoline-5.8-dione reacted with 2-aminopyridine derivatives, Out of the four possible products which could be achieved in this reaction. condensation and rearrangement product. 4a.10.11-triazabenzo［3.2-a］ fluorine-5.6-dione was obtained as major product. The definite structure was identified with X-ray crystallographic study. (omitted)

• Archives of Pharmacal Research
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• 제18권1호
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• pp.27-30
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• 1995

The Hantzsh reaction of 7-hydroxy-8-methoxy-2-oxo-2H-benzopyran-6-carboxaldehyde (1) with ethyl acetoacetate and ammonia yields the dihydropyridine derivative 2 together with the pyridine derivative 3 and the eight membred ring derivative 4. Reaction of 1 with ethyl cyanoacetate and malononitrile gives the iminodicoumarin derivatives 5 and 6 respectiely. The latter compound was reacted with butan-2-one and acetophenone to produce the Michael adduct 71, b and the 2-aminopyridine derivatives 8a, b.

• The Korean Journal of Physiology and Pharmacology
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• 제21권6호
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• pp.617-623
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• 2017

The vascular actions and mechanisms of taurine were investigated in the isolated human radial artery (RA). RA rings were suspended in isolated organ baths and tension was recorded isometrically. First, a precontraction was achieved by adding potassium chloride (KCl, 45 mM) or serotonin (5-hydroxytryptamine, 5-HT, $30{\mu}M$) to organ baths. When the precontractions were stable, taurine (20, 40, 80 mM) was added cumulatively. Antagonistic effect of taurine on calcium chloride ($10{\mu}M$ to 10 mM) -induced contractions was investigated. Taurine-induced relaxations were also tested in the presence of the $K^+$ channel inhibitors tetraethylammonium (1 mM), glibenclamide ($10{\mu}M$) and 4-aminopyridine (1 mM). Taurine did not affect the basal tone but inhibited the contraction induced by 5-HT and KCl. Calcium chloride-induced contractions were significantly inhibited in the presence of taurine (20, 40, 80 mM) (p<0.05). The relaxation to taurine was inhibited by tetraethylammonium (p<0.05). However, glibenclamide and 4-aminopyridine did not affect taurine -induced relaxations. Present experiments show that taurine inhibits 5-HT and KCl -induced contractions in RA, and suggest that large conductance $Ca^{2+}$-activated $K^+$ channels may be involved in taurine -induced relaxation of RA.

• Bulletin of the Korean Chemical Society
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• 제26권11호
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• pp.1701-1705
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• 2005

We have established an efficient method for the synthesis of the arylpiperazine derivatives in which the acylation of 2-aminopyridine, the coupling reaction of the acyl compound with piperazines, and reduction of the arylpiperazines were performed under a microwave irradiation (300 W) to afford the corresponding target compounds in quantitative yields. In all cases, the reaction times were remarkably reduced when compared with those of the conventional method.

• 약학회지
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• 제34권2호
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• pp.80-87
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• 1990

3-Substituted 5-aminoisoxazole-4-carboxylates were prepared by the reaction of corresponding bormoaldoximes with cyanoacetate. The 3-trifluoromethylisoxazole derivatives were acylated to amides with various aminopyridine derivatives to afford diamides. The ester group was hydrolyzed and decarboxylated easily to give 3-trifluoromethyl-5-aminoisoxazole. The aminoisoxazole was also converted to amides. 5-Amino-3-trifluoromethylisoxazole-5-one-4-carboxylate was prepared by the reaction of trifluoroacetoaldoximoyl bromide and malonate. 5-Amino-3-methylisoxazole-5-one-4-acetate was prepared by the reaction of hydroxylamine and acetylmalonate. The synthesized compounds were tested for antiinflammatory activities.

• 약학회지
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• 제34권6호
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• pp.422-428
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• 1990

2,3-Dibromo-1,4-naphthoquinone was reacted with p-aminobenzoic acid, 2-aminopyridine, 2-amino-4-metylpyridine, m-nitroaniline, sulfathiazol, p-chloroaniline, phenetidine and 2-bromo-3-(N-arylamino)-1,4-naphthoquinones($1{\sim}8$). 2,3-Epoxy-2,3-dihydro-1,4-naphthoquinone was also reacted with p-amonobenzoic acid, p-toluidine, p-chloroaniline, m-chloroaniline, m-nitroaniline, p-phenetidine, N,N-dimethyl-1,4-pheylenediamine as a ring opening and dehydogenation to form 2-hydroxy-3-(N-arylamino)-naphthoquinones ($9{\sim}16$) in good yield. These new compounds($1{\sim}16$) are expected to have a biological activities such as anticoagulant and cytotoxic.

• Archives of Pharmacal Research
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• 제15권4호
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• pp.317-321
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• 1992

Furoyldroximoyl chloride 3d reacted with 2-aminopyridine, 2-aminopyrimidine. O-aminophenol, O-phenylenediamine and aminothiophenol to afford imidazo [1, 2-a]pyridine 6. imidazo[1, 2-a]pyrimidine 8, benzoxadiazine 10, nitrosobenzopyrizine 13a and nitrosobenzothiazine 13b, respectively. Isoxazoline 18 and pyrrolidino[3, 4-d]isoxazolin-4, 6-dione derivatives 19a and 19b obtained by the reaction of 3 with acrylonitrile and N-arylmaleimide. Hydroximoyl chloride 3 reacted with thiophenol and sodium benzene-sulfinate to yield furylglyoxaloxime 16a and 16b, respectively. Hydroximoyl chloride 3 reacted also with some active methylene compound to give isoxazole derivatives 20-23, respectively.

• 약학회지
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• 제54권6호
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• pp.466-473
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• 2010

A series of $3{\beta}$-substituted 5-androstene-$17{\beta}$-carboxamides were synthesized from analogs of $3{\beta}$-hydroxy-5-androstene-$17{\beta}$-carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone $5{\alpha}$-reductase inhibitory activity of synthesized compounds was assessed by radioimmunoassay using [1,2,6,7-3H]-testosterone as substrate. All synthesized compounds showed lower activity than finasteride and the N-(3-pyridino)-$3{\beta}$-carboxycarbonyloxy-5-androstene-$17{\beta}$-carboxamide (12) showed weak inhibitory activity ($IC_{50}$: $2.4{\times}10^{-7}M$).

• Bulletin of the Korean Chemical Society
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• 제28권5호
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• pp.777-782
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• 2007

A novel library of amino-substituted 2-pyridones has been constructed through a two-step sequence of microwave-promoted Buchwald-Hartwig amination of 2-benzyloxy halopyridines followed by debenzylation. Microwave-promoted amination of 3- or 4-halopyridine in the presence of a suitable palladium catalyst and ligand system provided amino-substituted 2-benzyloxypyridines in excellent yields. Then, debenzylation of 2- benzyloxypyridines afforded the corresponding 2-pyridones with high efficiency.

• Archives of Pharmacal Research
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• 제14권4호
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• pp.319-324
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• 1991

2,6-Dimethyl-4-(3'-nitrophenyl)-3-methoxylaminocarbonyl-1,4-dihydropyridine-5-carboxylic acid methylester, 3b reacted with 2-cyanoethanol or benzylalcohol to give the corresponding cyanoethylurethane compound 6c in 40.6% yield and benzylurethane compound 6d in 32% yield. The cyanoethylurethane 6c was hydrolized in ethanolic NaOH to give 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methyl ester. HCl 8 in 64.8% yield. Another acid hydrolysis of benzylurethane 6d gave 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methylester. HBr 11 in 54.7% yield.