• Proceedings of the Zoological Society Korea Conference
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• 1994.10a
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• pp.216.1-216
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• 1994

• Bioindustry News
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• v.13 no.1
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• pp.28-35
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• 2000

• Bulletin of the Korean Chemical Society
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• v.18 no.12
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• pp.1242-1244
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• 1997

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.204-210
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• 1993

The distribution and excretion of DWC-751, a new cephalosporin, were examined in rats and mice following a single intravenous administration. DWC-751 in plasma and urine was determined by both HPLC and microbiological assay. The plasma concentration of the drug declined biexponentially. The initial and terminal half lives of the drug were 3.0 and 28.3 min, respectively. Binding of the drug to plasma proteins was 42.3%. The distribution volume at steacly-state ($Vd_{ss}$) was only 0.341 ι/kg, which is well correlated with the low n-octanol/water partition coefficient of the drug ($K_{o/w{\cong}0$) Actually, the drug was distributed to liver, kidney and lung with very low organ/plasma concentration ratio. The drug, was excreted mainly via renal excretion, i.e., the total($CL_T$) and apparent renal($CL_{R}$) clearances of the drug were 10.8 and 7.5 ml/min/kg, respectively.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.196-203
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• 1993

We compared in vitro antibacterial activity of DWC-751, a new parenteral cephalosporin antibiotic, with those of cefpirome (CPR), cefotaxime (CTX) and ceftazidime (CAZ). DWC-751 showed a broad antimicrobial spectrum against Gram-positive and negative bacteria. The antibacterial activity of DWC-751 against Stapylococcus aureus was equal to that of CPR and superior to those of CTX and CAZ. The activity of it against Excherichia coli was more potent than those of CPR, CTX and CAZ. Against Pseudomonas aeruginosa, DWC-751 was slightly inferior to that of CAZ and superior to those of CPR and CTX. The antibacterial activity of DWC-751 was superior to those of CPR, CTX and CAZ against clinical isolates and ofloxacin resistant strains. DWC-751 showed bactericidal action against Escherichia coli at concentrations close to the MIC and induced the formation of filament and burge and lysis of Escherichia coli in a microscopic examination.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.230-230
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• 1994

Human leukocyte elastase(HLE)는 폐와 피부, 혈관등의 Connective tissue의 주요 구성물인 elastin을 분해하는 효소로써, 백혈구의 식균작용에도 관여한다. 그러나 이효소가 과다하게 분비되면 pulmonary emphysema와 adult respiratory distress syndrome, rheumatoid arthritis를 유발한다고 알려지고 있다. 지금까지 HLE억제제로 시판되는 의약품은 없으나, 최근에 Cephalosporin유도체가 이 효소의 억제제로 우수한 효과가 있다는 보고가 있은 후, HLE억제제로써 이들의 유도체가 개발되고 있다. 연구자들은 다음일반식에서 2번과 3번위치에 치환기를 도입시킨 수종의 Cephalosporin Sulfone의 유도체들을 합성하고. 이들의 HLE억제 효과를 Spectrophotometerqkdtlr을 이용하여 측정하였다. 합성화합물증 몇가지는 우수한 HLE억제효과를 보여주었고, 2번위치에 diphenylcyclopropyl ring과 같은 부피가 큰 치환체를 도입하면 효소억제력이 증가되었다.

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.05a
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• pp.120-120
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• 2002

This study was designed to evaluate a repeated intravenous toxicity of a novel cephalosporin antibiotic, IDC7181, in Beagle dogs. Four groups, each consisting of 3 male and 3 female dogs (one year old, body weight 8 - 10 kg), were intravenously administered with IDC7181 at dose levels of 0 (vehicle control), 10, 50 or 250 mg/kg/day, respectively, for 28 days.(omitted)

• Biomolecules & Therapeutics
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• v.1 no.1
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• pp.103-108
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• 1993

The synthesis and physicochemical properties of a novel cephalosporin, DWC-751 are described. DWC -751, (6R , 7R)-7-[ (Z)-2-(2-aminothiazol-4-yl)-2- methoxyiminoacetamido]-3-[(1-methylbenzotriazol-3-ium) methyl]-ceph-3-em-4-carboxylate monosulfate($IV_{\alpha}$) was conveniently obtained by the conversion of compound (IV) into the crystalline monosulfate. Adjusting pH 4.8-5.2 in aqeous solution of the crude crystalline, compound(IV) in the form of a crystalline pentahydrate was prepared with a high degree of purity. The influence of the various organic and inorganic acids on the solubility of compoud(IV) and its salts, was examined. Particularly, the solubility of DWC-751 was 92 mg/mι at pH 1.7 and 233 mg/mι at pH 3.0. DWC-751 showed a broad antimicrobial spectrum against gram-positive and negative bacteria.

• Biotechnology and Bioprocess Engineering:BBE
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• v.2 no.2
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• pp.105-108
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• 1997

A search was undertaken to screen microorganisms that produce an enzyme capable of deacylating glutary1-7-amincephalosporanic acid to 7-aminocephalosporanic acid in soil samples. The screening was carried out by preparing enrichment cultures containing glutary-7ACA and cephalosporin C as selective carbon sources. A non-${\beta}$-lactam model compound,, glutary-p-nitroanilide, was synthesized as a substrate suitable for the rapid screening of microorganisms isolated from the enrichment cultures. Two isolates exhibiting acylase activity, designated BY7.4 and BY8.1, were identified as strains of Pseudomonas species. Pseudomonas BY8.1 showed higher acylase activity toward G1-7ACA than Pseudomonas BY7.4. Environmental conditions for the optimal acylase activity of Pseudomonas BY8.1 were shown to be pH9 and 30$^{\circ}C$.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.169-169
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• 2001

This study was designed to evaluate an acute and subacute intravenous dose toxicity of a new cephalosporin antibiotic agent, IDC-7181 in 7-week-old Sprague-Dawley rats. IDC-7181 was intravenously injected to rats at dose levels of 0, 3.2, 16, 80, 400 and 2, 000 mg/kg/day for single dose toxicity study and at dose levels of 0, 10, 50 and 250 mg/kg/day for 4 week-repeated dose toxicity study. All rats survived throughout the study periods.(omitted)