• Bulletin of the Korean Chemical Society
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• 제26권8호
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• pp.1190-1196
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• 2005

Halopyrroles, N-substituted 2-halopyrroles were prepared by halogenation of N-substituted pyrroles with NBS, NCS, or surfuryl chloride. N-Substituted 3-halopyrroles were synthesized by acid-catalyzed thermal and photochemical isomerization reactions of N-substituted 2-halopyrroles. Both the thermal and photochemical reactions were acid-catalyzed. For the acid-catalyzed isomerization, a mechanism of [1,3] bromine shift followed by deprotonation is operated. For the acid-catalyzed photoisomerization, an excited triplet state of 2-protonated N-benzyl-2-halopyrrole produces an intermediate N-substituted pyrrole complex with halonium ion which is equilibrated with N-substituted pyrrole plus halonium ion, and then the halonium ion newly adds to 3-position of N-substituted pyrrole followed by deprotonation to afford N-benzyl-3-halopyrrole.

• Archives of Pharmacal Research
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• 제29권11호
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• pp.1006-1017
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• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• Archives of Pharmacal Research
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• 제17권6호
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• pp.480-482
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• 1994

A number of 5-substituted pyrimidine acyclic nucleosides were synthesized and tested for invitor cytotoxicity against four cell lines (j-82 cell, p-388 cell, FM-3A cell and U-938 cell lines). Synthesis of 1-cyanomethyl-5-substituted pyrimidines (1a-e) and 1-(4-cyanobutyl)-5-substituted pyrimidines (2a-e) was acomplished from the series of alkylation reactions ofl 5-substituted uracils with the corresponding chloacetonitrile and 5-chlorovaleronitile in DMSO under $50^{\circ}C$ temperature. These 5-substituted pyrimidine acylic nucleosides (1a-e and 2a-e) exhibited moderate to significant acitivity aginst four cell lines.

• 대한화학회지
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• 제58권1호
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• pp.62-67
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• 2014

In the present study a novel series of (2-substituted-4-methylthiazol-5-yl)(4-substituted piperazin-1-yl)methanone derivatives were synthesized by reaction of 2-substituted-4-methylthiazole-5-carboxylic acid with N-substituted benzyl piperazine by using 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide hydrochloride (EDCl) and 1-hydroxybenzotriazole (HOBt) in DMF. All the newly synthesized compounds were characterized by spectral methods. The title compounds were screened for in vitro antibacterial activity. Most of the compounds show moderate to good antimicrobial activity.

• Archives of Pharmacal Research
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• 제17권6호
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• pp.420-423
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• 1994

Various N'-substituted anilino-N-methyl-N'-nitrosoureas(2a-n) were easily prepared from the reaction of substituted phenylhydraines $(3, 4-CH_3, {\;} 3-, {\;} 4-OCH_3, {\;} 3-, {\;} 4-F, {\;} 3, {\;} 4-Cl, {\;} 4-Br, {\;} 2-, {\;} 3-, {\;} 4-NO_2, 4-(NO_2)_2)$ with methyl isocyanate, followed by the nitrosation with 99% HCOOH and dry sodium lnitrite powder. Surprisingly, of these series of analogus, the anilino-nitrocosureas substituted with eletron-withdrawing nitro groups (2k-a) showed significantly low $ED_{30}$ values of $1.4-3.4 {\mu}g/ml.$ In addition, none of these copounds subtituted with electron-donating groups exhibited cytotoxicities.

• 한국축산식품학회지
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• 제21권1호
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• pp.38-46
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• 2001

This study was carried out to develop the processed cheese with the increase of unsaturated fatty acid by substituting different vegetable oils for the improvement of nutritional aspects without reducing its sensory advantage and texture properties. The texture properties(hardness, elasticity, adhesiveness, cohesiveness, brittleness and gumminess), meltability, fat leakage degree and sensory evaluation of the processed cheese were analyzed and compared. The meltability of the processed cheese was measured in the range from 59.7 to 138.3mm, the sample substituted with corn oil showed the lowest meltability but the sample substituted with butter resulted in the highest meltability. The degree of fat leakage had the range from 8.28 to 14.71$\textrm{cm}^2$. The sample substituted with safflower oil showed the lowest fat leakage degree but the sample substituted with butter had the highest fat leakage degree. The sample substituted with butter had the lowest hardness. There was no significant difference in the elasticity between the samples tested. The sample substituted with butter showed the lowest value in adhesiveness, cohesiveness, brittleness and gumminess, respectively. The preference score of the processed cheese samples ranged from 3.22 to 6.59. The texture score ranged from 3.12 to 3.26.

• 약학회지
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• 제31권1호
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• pp.14-18
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• 1987

2-Substituted-3, 4-dihydro-2H-1, 2-benzothiazin-4-one 1, 1-dioxide 6 was reatced with magnesium methyl carbonate to form magnesium chelate 7, which could be hydrolized in cold hydrochloric acid solution to give 2-substituted-4-hydroxy-2H, 1, 2-benzothiazine-3-Carboxylic acid 1, 1-dioxide 2 in good yield.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.250-257
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• 2002

A series of benzimidazole derivatives carrying different heterocycles such as 1,2,3-thiadiazole, 1,3,4-thiadiazole, thiazolidine, 2,3-dihydro-thiazole, 1,3,4-oxadiazole, semicarbazone and substituted thiosemi-carbazones were synthesized. Also a series of 1-methylbenzimidazole carrying hydroxy ethyl-amide, substituted sulfonyl hydrazide and benzoyl hydrazide from aminobenzoyl group at position 2 of 1-methylbenzimidazole were synthesized. The antimicrobial evaluation of some of the new compounds was carried out.

• Bulletin of the Korean Chemical Society
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• 제17권4호
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• pp.362-365
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• 1996

Carbonyl compounds 1, alkyl- and arylaldehydes and alkyl, aryl, benzylic, and cyclic ketones were converted to the corresponding 1,3-dioxolanes 2 and 1,3-dioxanes 4 with ethylene glycol and 2,2-dimethyl-1,3-propanediol in the presence of 1-3 mol% of 1-(p-substituted)benzyl-1,1-dimethyl-2-(p-substituted)-benzoyl hydrazinium hexafluoroantimonates 3 in high yields.

• 한국산학기술학회논문지
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• 제18권8호
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• pp.361-366
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• 2017

2개 논리식에 대해서 어떤 논리식 F의 일부가 다른 논리식 G 전체를 포함하고 있을 때, 논리식 F의 일부분을 논리식 G로 대치한 식을 대입식이라고 한다. 논리식 사이에 대입 관계가 성립되면 전체 논리식에 사용된 리터럴 개수를 대폭 줄일 수 있는 장점이 있으나, 대입 관계가 성립하지 않는 경우 대입식으로부터 얻을 수 있는 간략화 효과가 없게 되어 상대적으로 리터럴 개수를 줄이는 효과가 줄어들게 된다. 지금까지의 연구들이 주어진 논리식들 자체에 대해서 논리식들 사이의 대입 관계를 찾고, 대입이 가능하면 대입식을 산출하기 위한 방법을 제안하였는데, 본 논문에서는 논리식들 사이에 대입식이 만들어지도록 필요한 항을 추가하고, 다시 추가된 항들에 대한 보정을 통해 대입식을 산출하는 논리합성 방법을 제안한다. 최적화하고자 하는 2개의 논리식들로부터 항추가를 위한 행렬을 만들고, 행렬에서 항이 추가 가능한 묶음 찾고 추가된 항에 대해 보정을 하여 대입식이 완성된다. 실험결과 여러 벤치마크 회로에 대하여 제안한 방법이 기존 합성도구보다 리터럴 개수를 줄일 수 있음을 보였다.