• Bulletin of the Korean Chemical Society
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• 제11권5호
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• pp.383-386
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• 1990

We have synthesized several bicyclic heteroaromatic compounds with bridgehead nitrogen from N-amine salts of heteroaromatic amines. 2-Amino and 2-unsubstituted thiazolo[3,2-b][l,2,4]triazole derivatives 2a-b were prepared by the cyclization reaction from N-amine salts of aminothiazole-5-yl(N-methoxyimino)acetate with cyanogen bromide and formamidine acetic acid salt, respectively. 2-Methylthiazolo[3,2-b][1,2,4]triazole 2c was obtained from N-acetylated N-amine salt of aminothiazole-5-yl(N-methoxyimino)acetate by the cyclization reaction in the presence of polyphosphoric acid (PPA). 2-Substituted and 2-unsubstituted thiazole[3,2-b][1,2,4]triazole derivatives 2a-c were coupled with 7-aminocephalosporanic acid (7-ACA). Coupled cephalosporin derivatives 1a-c did not have good antibacterial activities in vitro.

• Bulletin of the Korean Chemical Society
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• 제32권spc8호
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• pp.2893-2894
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• 2011

• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1463-1464
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• 2010

• 약학회지
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• 제45권6호
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• pp.570-574
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• 2001

In order to discover new useful NSAIDs, novel N-substituted 1,2-benzisothiazoline-3-one 1,1- dioxide derivatives, which can exhibit potentially antiinflammatory activity were synthesized. 1,2-Benz-isothiazoline-3-one-N-acetic acids 6a, b were obtained from monochloroacetic acid and sodium 1,2-benz-isothiazoline-3-ones in DMF by N-alkylation reaction. N-Substituted 1,2-benzisothiazoline-3-one 1,1-dioxide derivatives 7a-e were synthesized through the coupling of compound 6a, b and several amines (aniline, 2- aminopyridine , 2-aminothiazole, 2-aminotetrazole) with dicyclohexylcarbodiimide in methyl e no chloride.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.189.1-189.1
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• 2003

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A$_3$ receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A$_3$ receptors. The most potent A$_3$ antagonist of the present series, N-［3-(4-methoxy-phenyl)-［1,2,4］thiadiazol-5-yl］-acetamide exhibiting a K$\_$i/ value of 0.79 nM at human adenosine A$_3$ receptors, showed antagonistic property in functional assay of cAMP biosynthesis involved in one of the signal transduction pathways of adenosine A$_3$ receptors. (omitted)

• 약학회지
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• 제44권4호
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• pp.318-324
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• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Bulletin of the Korean Chemical Society
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• 제11권4호
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• pp.323-327
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• 1990

The synthesis and some biological properties of $7{\beta} $-[2-(Z)-(2-aminothiazole-4-yl)-2-(N-substitutedcar bonyl)ethoxyiminoacetamido]-3-vinyl-3-cephem-4- carboxylic acid are described. The effect of substituents on the carbamoly group in the 7-side chain were investigated in order to improve antibacterial activities. Two of these new orally active $7{\beta} $-lactam derivatives showed wide expanded antimicrobial activities against Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa, as well as good stability to $7{\beta} $ -lactamases.

• 약학회지
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• 제44권2호
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• pp.155-161
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• 2000

New cephalosporin antibiotics , 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-7-[(1H-tetra-zol-1-yl)acetamido]-3-cephem-4-carboxylic acid 2, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl) oxymethyl]-7-[(2-aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid 3, 3-[(4-carb oxy-5-ethylthioisothiazol-3-yl)-oxymethyl]-7-[5-(ethylthio-3-hydroxyisothiazol-4-yl)carboxamido]-3-cephem-4-carboxylic acid 4, 3-[(4-car-boxy-5-ethylthioisothiazo1-3-yl)oxymethy1]-7-[(Z)-2-(fur-2-yl)-2-(methoxyimino)acetamido]-3-cephem-4-carboxylic acid 5, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(alkoxyimino)acetamido]-3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 6-8 were synthesized. Antibacterial activities and structure-activity relationships of these new cephalosporin derivatives were examined. Among them, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-5-ethylthylth-ioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 7 exhibited good antibacterial activities compared to cefotaxime and ceftriaxone.

• 약학회지
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• 제42권4호
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• pp.364-369
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• 1998

New cephalosporin antibiotics. 7-[(1H-tetrazolyl)acetamidol]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid trisodium salt 2,7-[(5-ethylthio-3-hydroxyisothiazol-4-yl)carbox-amidol-3-[(4-carboxy-3-hydroxyisothiazo1-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 3,7-[(2-aminothiazol-4-yl)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl]thiomethyl]-3-cephem-4-caboxylic acid 4,7-[(Z)-2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 5-9 were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and activities were examined. Among them, 7-((Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 8 and 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(l-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 9 exhibited good antibacterial activities compared with those of cefotaxime and ceftriaxone.

• Fibers and Polymers
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• 제3권1호
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• pp.43-48
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• 2002

A series of monoazo disperse dyes based on 2-amino-4-phenylthiazole was prepared using various N,N-dialkvlaniline derivatives as the coupling component. The dyes were characterized by IR spectral studies, visible absorption spectroscopy and elemental analysis. The dyeing performance of these dyes was assessed on cellulose triacetate and nylon fibers. These dyes were found to give a wide range of colour shades varying from bright red to royal blue with very good depth, brightness and levelness on fibers. The dyed fibers showed good to very good light fastness and very good to excellent fastness to washing, perspiration, rubbing and sublimation. The dyebath exhaustion and fixation on the fibers were found to be very good.