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C-3 및 C-7(치환) 세파로스포린계 항생제의 합성과 항균활성에 관한 연구(2)
河在天,高玉鉉,姜馨龍 조선대학교 약학연구소 1995 藥學硏究誌 Vol.17 No.1
In order to development new cephalosporin antibiotics 7β[(z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(1,5-dimethyl-2-pyrroletetrazol-2-yl]methyl-3-cephem-4-carboxylic acid(9) and 7β-[(z)-2-(2-aminothiazol-4-yl)-2-(methoxyimi no) acetamido]-3-[5-naphthyltetrazol-2-yl]methyl-3-cephem-4-carboxylic acid(10) were synthesized. These compounds were tested for antimicrobial activities in vitro against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341, Mycobacterium phlei IFO 3158, Alcaligenes faecalis KCTC 1004, Escherichia coli 8S, Salmonella typimurium KCTC 1925, Pseudomonas aeruginosa IFO 13130, Klebsiella pneumoniae KCTC 1560 and Candida albicans ATCC 10231, respectively. Compound(10) showed good antimicrobial activities against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Mycobacterium phlei IFO 3158 but compound(9) showed lower antimicrobial activities as compare with cefotaxime and cefazolin.
C_3 및 C_7위치에 치환된 새로운 세파로스포린 化合物의 合成과 抗菌活性(Ⅰ)
황화영,하재천,김영수,고옥현,강형룡 조선대학교 약학연구소 1994 藥學硏究誌 Vol.16 No.1
The synthesis and antimicrobial activity of cephalosporin having (Z)-2-(2-aminothiazol-4-yl)-2-trityloxyiminoacetamido group and 5-(2-chlorophenyl)-4-phenyl-4H-1, 2, 4-triazol-3-thiomethyl group on the C_3 and C_7 position of the cephem ring, respectively are descrived. This compound was tested for antimicrobial activity in vitro against Candida albicans ATCC 10231, Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341, Staphylococcus aureus ATCC 6538P, Mycobacterium phlei IIP-IPH, Escherichia coli KCTC 1039, Escherichia coli ESS, Klebisiella pneumoniae KCTC 1560, Salmonella typhymurium TV-119, Pseudomonas aeruginosa IFO 13130. The antimicrobial activity of synthetic compound was better as compare with cefotaxime and cefazoline against Micrococcus luteus ATCC 9341 & Escherichia coli KCTC ESS.
유지석(Ji Seak Yoo),하재천(Jai Chun Ha),고옥현(Ok Hyun Ko),유진철(Jin Cheol Yoo),강형룡(Hyung Ryong Kang) 대한약학회 1999 약학회지 Vol.43 No.3
To develop new cephalosporin antibiotics with improved antibacterial activities, a series of 7beta-[2-(2-aminothiazol-4-yl)-(Z)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(heterocycle)thiomethylpyrrolidin-3-ylthio]methyl-3-cephem-4-carboxylic acid (14-18) having aminothiazol carboxymethylethoxyimino group on the C-7 position and (heterocycle) thiomethyl pyrrolidinthiomethyl group on the C-3 position of the cephem ring were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. Compounds 15 and 16 showed remarkable antibacterial activity against Salmonella typhimurium TV119 and Alcalienes faecalis KCTC1004, but most of compounds showed lower activity than cefotaxime.
고옥현,강형룡,유진철,김경수,홍석순,김영수,황화영,하재천 조선대학교 약학연구소 1992 藥學硏究誌 Vol.14 No.1
7β[5-(Substituted) phenyl-2H-tetrazol-2-yl]acetamidocephalospranic acid, 7β-(5-Diphnenyl-methyl-2H-tetrazol-2-yl) acetamidocephalosporanic acid and 7β-[5-(Substituted)-4-phenyl-1.2.4-triazol2-yl]thioacetamidocephalosporanic acid were synthesized and tested in vitro antimicrobial activity. These compounds exhibited good antimicrobial activity against Gram-positive bacteria whereas most compounds showed decreased antimicrobial activity against Gram-negative bacteria
고옥헌(Ok Hyun Ko),홍석순(Sun Soon Hong),하재천(Jae Chun Ha),김영수(Young Soo Kim) 대한약학회 1994 약학회지 Vol.38 No.3
For the development new cephalosporin antibiotics with aminothiazolmethoxyimino moiety in the C-7 position and triazolthiomethyl moiety in the C-3 position of cephem ring, 7beta-[(z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(aryl or het.)-4-phenyl-4H-1,2,4-triazol-3-yl]thiomethyl-3-cephem-4-carboxylic acids were synthesized. These compounds were tested for antimicrobial activitiy in vitro against ten species of microorganisms. It showed remarkable antibacterial activity against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Escherichia coli ESS. The antibacterial activity of most new compounds showed more active than cefazoline, but these compounds were lower active than cefotaxime against Pseudomonas aeruginosa IFO 13130
3-(치환) 테트라조일메칠세파로스포린의 합성과 생리활성
고옥현(Ok Hyun Ko),김영수(Young Soo Kim),고봉석(Bong Suk Ko),이재영(Jae Young Lee),하재천(Jai Chun Ha),방희재(Hee Jae Bang),유진철(Jin Cheol Yoo),강형룡(Hyung Ryong Kang) 대한약학회 1998 약학회지 Vol.42 No.1
For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephem ring, 70-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.