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Aminothiazole Cephalosporin 계 항생물질의 합성
고옥현,강형룡 조선대학교 약학연구소 1998 藥學硏究誌 Vol.19 No.1
In order to develop new cephalosporin antibiotics with improved antimicrobial activities, 7-[(Z)-2-(aminothiazo1-4-y1)-2-(methoxyimino) acetamido]-3-[5-(4-methylthiophenyl) tetsazol-2-yl] thiocarbonylthiomethyl-3-cephem-4-carboxvlic acid and 7-[(Z)-2-(aminothiazo1-4-y1)-2-(methoxyimino) acetamido]-3-[5-(diphenyl methyl) tetrazol-2-yl] thiocarbonylthiomethy1-3-cephem-4-carboxylic acid were synthesized from 5-(4-methylthiophenyl) tetrazolyl-2- dithiocarbamate potassium salt or 5-(diphenylmethyl)tetrazolyl- 2-dithiocarbamate potassium salt and p-methoxybenzyl 7-[(Z)-2-(2- trity-laminothiazo1-4-yl)-2-(methoxyimino)acetamidol-3-chloromethyl-3-cephem-4-carboxylate, respectively.
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
고석태,강형룡 한국약제학회 1975 Journal of Pharmaceutical Investigation Vol.5 No.1
Polyporus would used as diuretics. Then, for the purpose of experimentally certifying the above mention, the effect on the renal function of dog was investigated, utilizing clearance technique. Water and alcohol extracts, when injected intravenously, produced significant increases of urinary sodium and potassium, osmolar and free water clearances, and urine flow, while glomerular filtration rate and renal plasma flow remained unchanged. During diuresis produced by furosemide, addition of water extract reduced the action of furosemide and markedly renal plasma flow. It would appear that these compounds are capable of action by a different mechanism or a different site. Water extract, when infused directly into a renal artery, reduced the urine flow of experimental kidney as well as renal plasma flow, and the contralateral kidney exhibited diuresis, whereas amounts of sodium and potassium excreted in urine increased on both kidney. It is surmised from those observations that Polyporus induces diuresis by inhibition the reabsorptive mechanism of renal tubules through some endogeneous humoral substances, in addition, directly reduces the renal plasma flow.
새로운 沆癌劑 2-Amino-4-thio(3H)pteridine 誘導體의 合成에 關한 硏究
高玉鉉,姜馨龍,金永洙,金成原 조선대학교 약학연구소 1983 藥學硏究誌 Vol.5 No.1
In order to obtain some new anticancer agents, authors synthesized N^4-(2-amino-3-cyano-5-methylpyrazine 1-oxide)-N^1-(4, 6-dimethyl-2-pyrimidinyl) sulfanilamide, N^4-(2-amino-3-cyano-5-methylpyrazine 1-oxide)-N^1-(2, 4-dimethoxy-4-pyrimidinyl) sulfanilamide, N^4-(2-amino-3-cyano-5-methylpyrazine 1-oxide)-N^1-(5-methyl-1.3.4-thiadiazol-2-yl)sulfanilamide by condensing 2-amino-3-cyano-5-chloromethylpyrazine 1-oxyide and sulfamethazine, sulfadimethoxine and sulfamethizole, respectively. we also synthesized N^4-〔2-amino-4-thio(3H)-6-methyl pteridine 8-oxide〕-N^1-(4, 6-dimethyl-2-pyrimidinyl)sulfanilamide, N^4-〔2-amino-4-thio(3H)-6-methylpteridine 8-oxide〕-N^1-(2, 4-dimethoxy-4-pyrimidinyl)sulfanilamide and N^4-〔2-amino-4-thio(3H)-6-methylpteridine 8-oxide〕-N^1-(5-methyl-1.3.4-thiadiazol-2-yl)sulfanilamide, respectively.
Quaternary Ammonium Salt Cephalosporin계 抗生劑 合成
高捧奭,高玉鉉,姜馨龍 조선대학교 약학연구소 1995 藥學硏究誌 Vol.17 No.1
For the development of quaternary ammonium salt cephalosporin antibiotics with improved antimicrobial activities, a series of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(methox yimi no) acetamido]-3-[4-alkyl (or aryl)-3- thiosemicarbazid-1- nicotinonium] methyl -3- cephem -4- carboxylate were synthesized. Antimicrobial activities of these new compounds were examined against Gram(+) and Gram(-)bacteria. It was found that the moiety synthesized cephalosporin derivatives were good antibacterial activities against Escherichia coli. Almost these compounds were more antibacterial activities than cefazoline. These new compounds showed lower activity than cefotaxime against Pseudomonas aeruginosa.
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.