• Title/Summary/Keyword: 1-chloro-2

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Skin Irritation and Sensitization Studies on a Disinfectant Composed of 4-Chloro-m-cresol, Didecyl Dimethyl Ammonium Chloride, and Glutaraldehyde for the Bactericide (4-Chloro-m-cresol, Didecyl Dimethyl Ammonium Chloride 그리고 Glutaraldehyde로 구성된 살균 소독제에 대한 피부 자극성 및 감작성 시험에 관한 연구)

  • Chung, Hee-Sik;Kim, Suk;Chung, Myung-Sun;Jung, Won-Chul;Kim, Dong-Hyeok;Lim, Jeong-Ju;Shon, Ho-Yeong;Kim, Moo-Suk;Kim, Gon-Sup;Lee, Hu-Jang
    • Journal of Food Hygiene and Safety
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    • v.22 no.2
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    • pp.110-115
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    • 2007
  • This test was performed to evaluate the skin irritation and sensitization of Creocomplex, disinfectant, Containing 10% 4-chloro-m-cresol, 10% didecyl dimethyl ammonium chloride, and 10% glutaraldehyde. In primary skin irritation test, rabbits were dermally treated with Creocomplex for 24 hrs. The disinfectant did not induce any adverse reactions such as erythema and edema on intact skin sites, but on abraded skin sites, some rabbits showed very slight erythema and edema 24hr after topical application. So, the disinfectant was classified as a practically non-irrifating material based on the score 0.13 of primary irritation index. In the skin sensitization test, guinea pigs were sensitized with intradermal injection of 0.1ml Creocomplex for 24 hr. After 1 week, Creocomplex was treated on the site of injection, and challenged 2 weeks later. Creocomplex did not induce any allergic reactions. Therefore, 10% Creocomplex was graded as a weak material from 0 in both sensitization score· and rate. From results of the present study, it is suggested that 10% Creocomplex does not cause contact irritation and sensitization.

Synthesis of Certain Mercapto and Aminopyrimidine Derivatives as Potential Antimicrobial Agents

  • El-Kerdawy, M.M.;Eisa, H.M.;El-Emam, A.A.;Massoud, M.A.;Nasr, M.N.
    • Archives of Pharmacal Research
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    • v.13 no.2
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    • pp.142-146
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    • 1990
  • Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.

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Synthesis of Nucleophilic Adducts of Thiols(II). Addition of Thioglycolic Acid to ${\beta}$-Nitrostyrene Derivatives (Thiol의 친핵성 첨가물의 합성 (제2보). ${\beta}$-nitrostyrene 유도체에 대한 Thioglycolic Acid의 친핵성 첨가반응)

  • Tae-Rin Kim;Tae-Sung Huh;In-Sup Han
    • Journal of the Korean Chemical Society
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    • v.25 no.6
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    • pp.390-393
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    • 1981
  • Eight new compounds were prepared by the addition reaction of thioglycolic acid to ${\beta}$-nitrostyrene and its derivatives. s-[2-Nitro-1-phenylethyl]-thioglycolic acid; s-[2-nitro-1-(p-methyl)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(p-methoxy)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(p-chloro)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(p-bromo)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(p-nitro)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(3-methoxy-4-ethoxy)phenylethyl]-thioglycolic acid; s-[2-nitro-1-(3,4,5-trimethoxy)phenylethyl]-thioglycolic acid; The structure of these compound were identified by elemental analysis, UV, IR and NMR spectral data.

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CoMFA and CoMSIA on the Neuroblocking Activity of 1-(6-Chloro-3-pyridylmethyl)-2-nitroiminoimidazolidine Analogues

  • Sung, Nack-Do;Jang, Seok-Chan;Choi, Kyoung-Seop
    • Bulletin of the Korean Chemical Society
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    • v.27 no.11
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    • pp.1741-1746
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    • 2006
  • 3D-QSARs on the neuroblocking activities by 1-(6-chloro-3-pyridylmethyl)-2-nitroiminoimidazolidine analogues as agonist at the nicotinic acetylcholine receptor (nAChR) were studied quantitatively using CoMFA and CoMSIA methodologies. The statistical results of CoMFA (A5: $r^2\;_{cv.}\;=\;0.707\;&\;r^2\;_{ncv.}$= 0.986) and CoMSIA model (A3: $r^2\;_{cv.}$ = 0.715 & $r^2\;_{ncv.}$ = 0.961) showed the best predictability and fitness for neuroblocking activity based on the cross-validated value and non-cross validated value. The steric and H-bond acceptor nature of a compound were essential for high activity. The study on 3D-QSARs between substrate molecules and their neuroblocking activities appears to be an useful approach for designing better neuroblocking drug development.

Synthesis of 2-(Pyrazol-1-yl)quinoxalines and 2,3-Di(pyrazol-1-yl)quinoxalines (2-(Pyrazol-1-yl)quinoxaline류 및 2,3-Di(pyrazol-1-yl)quinoxaline류의 합성)

  • Kim, Ho-Sik;Jeong, Won-Young;Choi, Kyung-Ok;Lee, Seong-Uk;Kwag, Sam-Tag;Lee, Man-Kil
    • Journal of the Korean Chemical Society
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    • v.46 no.1
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    • pp.37-45
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    • 2002
  • The reaction of 3,6-dichloro-2-(3,5-dimethylpyrazol-1-yl)quinoxaline(8) or 6-chloro-3-hydrazino-2-(3,5-dimethylpyrazol-1-yl)quinoxaline(9) with substituted anilines, sulfa drugs and heteroacyl chlorides gave 2-(pyrazol-1-yl)quinoxalines(10-12). The reaction of compound 9 with alkyl (ethoxymeth-ylene) cyanoacetates resulted in the intramolecular cyclization to give 2,3-di(pyrazol-1-yl)quinoxalines(13).

Synthesis of 2-Cyanoimino-1,3-thiazoline (2-Cyanoimino-1,3-thiazoline 유도체의 합성)

  • Hahn, Hoh-Gyu;Nam, Kee-Dal;Park, Ik-Kyu;Mah, He-Duck
    • The Korean Journal of Pesticide Science
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    • v.7 no.2
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    • pp.155-158
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    • 2003
  • 2-Imino-1,3-thiazolines 1 show selective antifungal activity against pyricularia oryzae by new mode of action. A synthesis of novel 2-cyano-l,3-thiazolines 2 in which cyano moiety is substituted in imino group at C-2 of 1 is described. The lone pair electrons of sulfur and nitrogen as well as strong electron withdrawing cyano substituent in 1,3-thiazoline scaffold would effect the biological activity of 2-imino-1,3-thiazoline series. Regiospecific nucleophilic attack of thiourea 4 for $\gamma$-chloro-$\beta$-ketoacetoacetanilide 3 followed by acid catalyzed dehydration gave 2.

새로운 Quinolone 항균제 개발 연구

  • 함원훈
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.118-118
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    • 1993
  • 퀴놀론 모핵의 합성은 기존에 알려진 합성 방법인 Could-Jacobs방법과 Bayer방법에 의해서 Intermediate로 사용된 7-chloro-1-ethyl-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid와 1-cyclopropyl-7-chloro-6-Fluoro-1,4-dihydro-4-oxoquinolne-3-carboxylic acid를 합성하였다. Heteroaromatic tin compound는 furan, thiophene, 3-bromopyridine, 2-fluoropyridine에 n-BuLi을 사용하여 metallation 한후 electrophile로 tributyltin chloride를 사용하여 2-tributylstannofuran, 2-tributylst-annothiophene, 3-tributylstannopyridine, 2- fluoro-2-tributylstannop-yridine을 합성할 수 있었다. 이상의 Intermediate와 tin compounds를 p-alladium 촉매하에서 반응시켜 1-ethyl-7-(2-furanyl)-6-fluoro-1,4-dihy-dro-4-oxo-3-quinoline-carboxylic acid (compound 3), 1-ethyl-7-(2-th-iophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinol in carboxylic acid(compound 5), 1-ethyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 7), 1-ethyl-7-(2-fluoro-3-pyrid-nyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 9), 1-cyclopropyl-7-(2-furanyl) -6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 4), 1-cyclopropyl-7-(2-thiophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 6) ,1-cyclopropyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 8), 1-cyclopropyl-7-(2-fluoro-3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 10)를 합성하였다.

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Studies on the hemolytic mechanism of the 2-Chloro-3-(p-carboxyanilino) -1, 4-naphthoquinone derivatives (2-Chloro-3-(p-carboxyanilino)-1, 4-naphthoquinone 유도체의 용혈기전에 관한 연구)

  • 최병기;조정희;배경아;정세영
    • Environmental Analysis Health and Toxicology
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    • v.8 no.3_4
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    • pp.13-21
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    • 1993
  • In order to evaluate the anticancer activity of 1,4-naphthoquinone derivatives, several 1,4-naphthoquinone derivatives were newly synthesized and subjected to mouse leukemia p-388 cell line by MTT cytotoxicity assay. Among the several 1,4-naphtho-quinone derivatives, YC-001 has showed the most potent anticancer activity. To determine the safety of YC-001, hematotoxicity was tested. YC-001 induced hemolysis increased with both concentration and time dependent manner. The mechanism of hemolysis considered to be the generation of oxygen free radicals and lipid peroxydation of erythrocyte membrane which composed of phospholipids. Also methemoglobin, oxidized form of hemoglobin, was formed by YC-001.

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Crystal Structure Analysis of N,N'-bis(3-chloro-2-methylsalicylidene)-1,4-butanediamine

  • Sharmila, P.;Rajesh, R.;Venkatesan, R.;Ganapathy, Jagadeesan;Aravindhan, S.
    • Journal of Integrative Natural Science
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    • v.9 no.4
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    • pp.255-260
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    • 2016
  • The crystal structure of the saliciline derivatives N,N'-bis(3-chloro-2-methylsalicylidene)-1,4-butanediamine ($C_{20}H_{22}Cl_2N_2O_2$) has been determined from single crystal X-ray diffraction data. In the title compound crystallizes in the triclinic space group $P{\bar{i}}$ with unit cell dimension $a=4.6085(3){\AA}$, $b=5.9747(3){\AA}$ and $c=5.9747(3){\AA}$ [${\alpha}=83.889(4)^{\circ}$, ${\beta}=86.744(5)^{\circ}$ and ${\gamma}=82.085(5)^{\circ}$]. The title compound is essentially planar conformation. The compound lies across a crystallographic inversion centre and adopts E configurations with respect to the C-N bonds. The crystal packing of the molecules of compound is stabilized through weak O-H...N intra molecular interactions