• 제목/요약/키워드: 3-carboxylic acid

검색결과 438건 처리시간 0.026초

Piperazinyl Quinolone계 유도체의 합성 및 항균작용 (Synthesis and Antimicrobial Activities of Piperazinyl Quinolone Derivatives)

  • 임철부;이영운;최수항;염정록;허인회
    • 약학회지
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    • 제35권6호
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    • pp.515-521
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    • 1991
  • A number of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-substitutedcarbamyl-1-piperazinyl) quinoline [or 1,8-naphthyridine]-3-carboxylic acid and their pivaloyloxymethyl esters were prepared. The compounds synthesized were evaluated for antibacterial activity in vitro against Escherichia coli, Bacillus subtilis, Proteus vulgaris, Klebsiella pneumoniae, Staphylococcus aureus and Pseudomonas aeruginosa. Among those 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-methylcarbamyl-1-piperazinyl) quinoline-3-carboxylic acid [1] and 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-methylcarbamyl-1-piperazinyl)1,8-naphthyridine-3-carboxylic acid [6] showed the most potent in vitro antibacterial activity.

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7-[(3-메틸티오 또는 3-메틸티오메틸)피롤리디닐]퀴놀론-3-카르복실산의 합성과 항균작용 (Synthesis and Antimicrobial Activity of 7-[(3-Methylthio or 3-Methylthiomethyl)pyrrolidinyl] quinolone-3-carboxylic Acid)

  • 이재욱;강태충;이규삼;손호정;윤길중;유영효;김대영
    • 약학회지
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    • 제38권2호
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    • pp.197-201
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    • 1994
  • A number of 7-[(3-methylthio or methylthiomethyl)pyrrolidiny]qui nolone-3-carboxylic acids were synthesized by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthiopyrrolidine or 3-methylthiomet hylpyrrolidne. 3-Methylthiopyrrolidine or 3-methylthio-methylpyrrolidine which was prepared from N-benzyl-3-hydroxy pyrrolidine or 3-hydroxymethylpyrrolidine. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microorganisms. Among those 1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethy-lpyrrolidinyl)-1,4-d ihydro-4-oxo-3-quinolinecarboxylic acid(7d) and 1-cyclopropyl-6- fluoro-8-chloro-7-(3-methylthiomethyl pyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (7f) showed the most potent in vitro antibacterial activity.

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2,2'-(ethylenediimino) and 2,2'-(thioureido)-di-1-carboxylic acids의 항결핵성및 항균성화합물로서의 합성연구 (Synthetic studies of 2,2'-(ethylenediimino) and 2,2'-(thioureido)-di-1-carboxylic acids as the antitubercular and the other bacteriostatic agents)

  • Chough, Yun-Sung
    • 약학회지
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    • 제10권2_3호
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    • pp.8-11
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    • 1966
  • 항인결핵균성및 streptomycin, isoniazid및 para-aminosalicylic acid에 대한 내성인결핵균주에 현저한 항균작용 있는 dextro-2,2'-(ethylenediimino)-di-1- butanol(Ethambutol) 계열 및 thioureido(-NHCSNH-) 함유화 합물 계열인 2,2'-(ethylenediimino)-di-1-butyric acid및 2,2'-(thioureido)-di-1-butyric acid를 합성했으며 이들 약물의 구조와 작용간의 상호관계를 설명코저 이들 화합물과 류사한 구조인 2,2'-(thioureido)-di-acetic acid를 합성했기에 보고함.

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Biosynthesis of L-Azetidine-2-carboxylic acid in actinoplanes ferrugineus

  • Lee, Kang-Man;Woodard, Ronald W.
    • 미생물과산업
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    • 제13권1호
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    • pp.10-13
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    • 1987
  • L-Azetidine-2-carboxylic acid(A-2-C) is a four-membered cyclic imino acid which was first discovered from Convalaria majalis and Polygonatum officinalis in 1955(1,2). The imino acid A-2-C has been identified in at least 16 species of plants (3) (mostly the families Liliaceae, Agavaceae and Amaryllidaceae); in two marine sponges (Haliclona sp. and Chalinospilla sp.) (4); in the red algae (Lophocladia lamenandi) (5); in the sugar beet Beta vulgaris (6) ; and the microorganism Actinoplanes ferrugineus (7).

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Synthesis and In Vitro Cytotoxicity of 1,3-Dioxoindan-2-Carboxylic Acid Arylamides

  • Jung, Jae-Kyung;Ryu, Jin-Hyeong;Yang, Sung-Il;Cho, Jung-Sook;Lee , Hee-Soon
    • Archives of Pharmacal Research
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    • 제27권10호
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    • pp.997-1000
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    • 2004
  • A series of 1,3-dioxoindan-2-carboxylic acid arylamides were synthesized and evaluated for in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T- 47D). The most active was compound 3e (1.2 ${\mu}M$ against SK-OV-3 cell line) bearing a 4- methyl substituent.

${\beta},\;{\gamma}$-불포화카르복시산, 카르복시아미드와 니트릴 유도체의 합성과 이들의 광화학적 반응에 관한 연구 (Synthesis and Exploratory Photochemistry of ${\beta},\;{\gamma}$-unsaturated Carboxylic Acid, Carboxamide and Nitrile Derivatives)

  • ;채우기
    • 대한화학회지
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    • 제26권2호
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    • pp.99-106
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    • 1982
  • 1-아세틸-1-메틸-2-시클로펜텐 화합물의 케톤 Chromophore를 나트릴, 카르보시산, 아미드 등의 group으로 대치하여 이들의 광화학반응을 검토한 결과 케튼 Chromophore에서 볼 수 있는 1,3-Acyl shift나 ODPM 반응은 일어나지 않았고 광화학적 중합 및 환원반응등 Chromophore를 변화시키므로서 광화학반응에 큰 변화를 보여주었다. 1-Cyano-1-methyl-2-cyclohexene의 경우도 Ketone chromophore와 비교하여 광화학 반응을 검토하였다.

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앉은부채(Symplocarpus renifolius Schott) 뿌리의 성분 (Constituents from the Root of Symplocarpus renifolius Schott)

  • 염정록;박동우
    • 생약학회지
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    • 제28권3호
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    • pp.143-148
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    • 1997
  • From the root of Symplocarpus renifolius, four compounds were isolated and their structure was elucidated by chemical and spectroscopic methods. They were identified as ${\beta}-sitosterol$ (compound 1), asparagine (compound 2), isocorydine (compound 3) and 3-hydroxymethyl-4-phenyl phenoxy carboxylic acid glucopyranosyl ester (compound 4). These compounds were firstly isolated from roots of Symplocarpus renifolius. Compound 4 was identified as a new compound, named as symplocarposide.

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세팔로스포린 3'-퀴놀론의 합성 및 항균작용 (Synthesis and Antibacterial Activity of Cephalosporin 3'-Quinolone Dithiocarbamate)

  • 나성범;정명희;김완주;지웅길
    • 약학회지
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    • 제37권2호
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    • pp.136-142
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    • 1993
  • To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

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