• Archives of Pharmacal Research
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• 제14권3호
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• pp.266-270
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• 1991

Synthesis of C-(2-furyl)-N-(4-nitrophenyl)methanohydrazonyl bromide 2 is described. Treatment of 2 with uncleophiles affords the corresponding substitution products 3-7. Also, compound 2 reacts with selenocyanate anion and thiocyanate anion and give the corresponding selenadiazoline and thiadiazoline 8 and 9, respectively. Moreover, reaction of 2 with enolates of various active methylene compounds afforded the pyrazole derivatives 17-20.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.495-501
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• 2004

A series of N-substituted-1,3-isoindolinedione derivatives (2-16) were synthesized for the purpose of defining the effect of N-substitution on the anticonvulsant activity of these derivatives. The target compounds (2-16) were obtained by condensation of phthalic anhydride with the corresponding amine derivative. The structures of the synthesized derivatives (2-16) were confirmed by means of IR, $^1$H-NMR, $^{13}$ C-NMR, MS and elemental analyses. The anticonvulsant activity of all compounds (2-16) were evaluated by subcutaneous pentylenetetrazole seizure threshold test at doses of 0.2, 0.4 and 0.8 mmol/kg compared with sodium valproate as a positive control. Their neurotoxicity were determined by the rotorod test. Many of the present series of compounds showed good anticonvulsant activity at the tested doses, as compared to sodium valproate. Three of them (4, 6 and 11) exhibited 100 % protection against convulsions, neurotoxicity and death at all tested doses. Out of the series, two compounds (12 and 13) were completely inactive with 100% mortality. 3-(p-chlorophenyl)-4-(1 ,3-dioxo-2,3-dihydro-1 H-2-isoindolyl) butanoic acid derivative (11) has emerged as the most active compound which is 20 times more active than valproate with ED$_{50}$ 8.7, 169 mg/kg; TD$_{50}$ 413, 406 mg/kg and PI 47.5, 2.4. The results revealed the importance of the combination of baclofenic and phthalimide moieties (compound 11) as a promising anticonvulsant candidate.

• Archives of Pharmacal Research
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• 제27권6호
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• pp.610-614
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• 2004

The in vitro antioxidant properties of some flavone-6(4)-carboxaldehyde oxime ether deriva-tives (Ia-f, lIa-f） were determined by their effects on the rat liver microsomal NADPH-dependent lipid peroxidation (LP） levels by measuring the formation of 2-thiobarbituric acid reactive substances. The free radical scavenging properties of the compounds were also examined in vitro by determining their capacity to scavenge superoxide anions and interact with the stable free radical 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The most active compounds, lib (Flavone-4＇-carboxaldehyde-O-ethyl oxime） and Id (Flavone-6-carboxaldehyde-O-［2-(1-pyrolidino） ethyl］ oxime）, caused 98 and 79％ inhibition of superoxide anion production and DPPH stable free radical at $10^{-3}{\;}M$, respectively.

• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.131-136
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• 2011

Synthesis of N-(1H-benzimidazol-2-yl)-6-substituted-1,3-benzothiazol-2-amines and 6-substituted-N-(4,5-dihydro-1H-imidazol-2-yl)-1,3-benzothiazol-2-amines by the reaction of substituted 2-aminobenzothiazoles with carbon disulphide and methyl iodide followed by the reaction with o-phenylene diamine/ethylene diamine are reported. All the synthesized compounds were characterized by elemental analysis, IR spectra and $^1H$ NMR spectral studies. The potent antibacterial and entomological (antifeedant, acaricidal, contact toxicity and stomach toxicity) activities of the synthesized compounds were investigated.

• 생약학회지
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• 제38권2호통권149호
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• pp.164-169
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• 2007

ln our continued search for biologically active compounds from traditional medicine, we found that ethyl acetate fraction from Inonotus obliquus showed potent antioxidant activities on three different cell-free bioassay systems. Bioassay-directed chromatographic fractionation of the ethyl acetate fraction from Inonotus obliquus afforded four phenolic compounds, 4-(3,4-dihydroxyphenyl)-(E)-3-buten-2-one (1) , 3,4-dihydroxybenzaldehyde (2), protocatechuic acid (3) and caffeic acid (4) along with three sterols such as lanosterol (5), ergosterol peroxide (6) and 9,11-dehydroergosterol peroxide (7). Among isolates, phenolic compounds (1-4) were assessed for antioxidant activities. Almost phenolic compounds showed potent DPPH and superoxide anion radicals scavenging and lipid peroxidation inhibitory activities indicating that these phenolic compounds contribute to the antioxidative activities of I. obliquus. Compounds 2-3 and 7 were isolated for the first time from this plant.

• Archives of Pharmacal Research
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• 제17권2호
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• pp.87-92
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• 1994

A series of $7-{2-(aminothiazol-4-yl)-2-Z-({\gamma}-lacton-3-yl)oxyiminoactamido}$ cephalosporins with various substituents at the 30position in cephem nucleus in cephem nucleus were synthesized and evaluated microbiologically. The tested compounds showed potent activities but were somewhat less active than cefotaxime or cefixime against a wide variety of Gram-positive and Gram-negative bacteria.

• Archives of Pharmacal Research
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• 제29권1호
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• pp.26-33
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• 2006

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

• 약학회지
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• 제17권1호
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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.

• 약학회지
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• 제45권6호
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• pp.565-569
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• 2001

Five novel cinmetacin amide derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity was compared with cinmetacin. Cinmetacin and hydroxysuccinimide were reacted with dicyclohexyl carbodiimide to give cinmetacin active ester (4), which was treated with amines to yield cinmetacin amides (5-9). Compounds (5) and (9) gave stronger analgesic activity than cinmetacin and compounds (5), (6), (9) showed comparable antiinflammatory activity to cinmetacin.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.51-55
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• 1995

A facile convenient syntheses of the titled compounds, via reacting the precusor 2-amino-2-(pentane-2, 4-dion-3-yithio)-6-phenylpyrimidine-5-carbonitrile (1) with nitrogen nucleophiles and with the carbanions of some active methylene compounds, is reported. Chemical and spectroscopic evidence of the newly syntheised compounds are described.