• Title/Summary/Keyword: 7-ACA

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In vivo Evaluation of a Novel ${\beta}-Lactam$ Antibiotics, YH-487 (새로운 ${\beta}-Lactam$계 항생물질 YH-487의 in vivo 항균활성)

  • Won, Yu-Jung;Kang, Heui-Il;Lee, Jong-Wook;Chung, Dong-Hyo
    • Applied Biological Chemistry
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    • v.40 no.2
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    • pp.157-162
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    • 1997
  • A novel compound, named YH-487, was synthesized by attaching the thiol and aminothiazole residue to $C_3$ and $C_7$ position of 7-aminocephalosporanic acid (7-ACA). The therapeutic efficacy on infected animals, pharmacokinetics in vivo and the effect on intestinal microflora of YH-487 were examined. The pharmacokinetics of YH-487 were similar to that of cefotaxime, a third generation ${\beta}-lactam$ antibiotics, in rat. Upon in vivo administration, YH-487 was predominantly delivered to kidney, and mostly excreted through kidney without making any metabolites. The therapeutic efficacy of YH-487 to animal infected with E. coli was three times and twenty times higher than that of cefotaxime and cefotiam, respectively, In vivo administration of YH-487 to Sprague-Dawley rats significantly decreased the population of intestinal gram negative species such as Enterobacteria and Barteroides. However, no significant changes were obseved in gram positive species such as Lactobacillus, Bifidobacteria and Staphylococcus. In addition, continuous administration of YH-487 did not increase the possibility to induce resistant strains in intestinal microflora.

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A Study on the Synthesis and Antibacterial Activities of 3-[(4-Carboxy-5-ethylthioisothiazo1-3-yl) oxymethyl] cephalosporin Derivatives (3-[(4-카르복시-5-레틸티오이소티아졸-3-일)옥시메틸] 세파로스포린 유도체들의 합성 및 항균력에 관한 연구)

  • 최원식;박의석;박규종;이영행
    • YAKHAK HOEJI
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    • v.44 no.2
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    • pp.155-161
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    • 2000
  • New cephalosporin antibiotics , 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-7-[(1H-tetra-zol-1-yl)acetamido]-3-cephem-4-carboxylic acid 2, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl) oxymethyl]-7-[(2-aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid 3, 3-[(4-carb oxy-5-ethylthioisothiazol-3-yl)-oxymethyl]-7-[5-(ethylthio-3-hydroxyisothiazol-4-yl)carboxamido]-3-cephem-4-carboxylic acid 4, 3-[(4-car-boxy-5-ethylthioisothiazo1-3-yl)oxymethy1]-7-[(Z)-2-(fur-2-yl)-2-(methoxyimino)acetamido]-3-cephem-4-carboxylic acid 5, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(alkoxyimino)acetamido]-3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 6-8 were synthesized. Antibacterial activities and structure-activity relationships of these new cephalosporin derivatives were examined. Among them, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-5-ethylthylth-ioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 7 exhibited good antibacterial activities compared to cefotaxime and ceftriaxone.

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Synthesis and Antibacterial Activities of 3-[(4-Carboxy-3-hydroxyisothiazol-5-yl)thiomethyl] cephalosporin Derivatives (3-[(4-카르복시-3-히드록시이소티아졸-5-일)티오메틸] 세파로스포린 유도체들의 합성 및 항균력)

  • Lee, Young-Haeng;Park, Kyu-Jong;Kim, Ha-Jung;Choi, Won-Sik
    • YAKHAK HOEJI
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    • v.42 no.4
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    • pp.364-369
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    • 1998
  • New cephalosporin antibiotics. 7-[(1H-tetrazolyl)acetamidol]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid trisodium salt 2,7-[(5-ethylthio-3-hydroxyisothiazol-4-yl)carbox-amidol-3-[(4-carboxy-3-hydroxyisothiazo1-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 3,7-[(2-aminothiazol-4-yl)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl]thiomethyl]-3-cephem-4-caboxylic acid 4,7-[(Z)-2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 5-9 were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and activities were examined. Among them, 7-((Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 8 and 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(l-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 9 exhibited good antibacterial activities compared with those of cefotaxime and ceftriaxone.

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Studies on the Synthesis and Antibacterial Activities of 7-Thiazinylcephalosporin Derivatives (7-티아지닐 세파로스포린 유도체의 합성과 생리활성에 관한 연구)

  • Lee, Young-Haeng;Chai, Kyu-Yun;Hyang, Sun-Am;Choi, Won-Sik
    • YAKHAK HOEJI
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    • v.41 no.4
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    • pp.473-479
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    • 1997
  • New cephalosporin antibiotics, 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-substituted-3-cephem-4-carboxylic acid derivatives 2a-2d, 7 -[(3,4-dihydro-6-ethoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido] -3-substituted-3-cephem-4-carboxylic acid derivatives 3a-3d and 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl-1-(S)-oxide)acetamido]-3-substituted-3-cephem-4-carboxylic acid derivatives 4a-4d were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and their activities were examined. Among them, 7-[(3,4-dihydro-6-methoxycaronyl-2,2-dimethyl-2H-1,4-thiazin-3-yl-1-(S)oxide)-acetamido]-3-[(1,2,3-triazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid 4d exhibited the antibacterial activities against Gram(+)and Gram(-) bacteria.

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Transcranial Doppler Detection of Vasospasm Following Subarachnoid Hemorrhage (지주막하 출혈에 따른 Vasospasm에 대한 Transcranial Doppler의 임상적 적용)

  • Lee, Jun Hong
    • Annals of Clinical Neurophysiology
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    • v.1 no.1
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    • pp.55-59
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    • 1999
  • Vasoconstriction of intracerebral arteries is the leading cause of delayed cerebral infarction and mortality following aneurysmal subarachnoid hemorrhage. Transcranial Doppler studies show and increase in the flow velocities of basal cerebral arteries, which usually start around day 4 following a subarachnoid hemorrhage, and peaking by days 7 to 14. Angiographic studies confirm the presence of at least some degree of MCA vasospasm when the flow velocities are higher than 100 cm/sec. Mean velocities in the 120 to 200 cm/sec range correspond to 25 to 50% luminal narrowing. MCA and ACA vsospasm is detected with around 90% specificity. Sensitivity is 80% and 50% respectively. A 200cm/sec threshold and rapid flow velocity increase exceeding 50 cm/sec on consecutive days, has been associated with subsequent infarction. Transcranial Doppler is also used to monitor the effects of endovascular treatment of vasospasm. Flow velocities decrease following successful angioplasty or papaverine infusion. Overall, transcranial Doppler studies are considered to have acceptable accuracy for the evaluation of vasospasm in aneurysmal subarachnoid hemorrhage, with limitations that have to be taken into consideration in the clinical setting.

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Analysis on Ischemic Cerebrovascular of Middle Age and Oldest-Old Age by Using Magnetic Resonance Imaging (자기공명영상을 이용한 중년 및 초고령의 허혈성 뇌혈관 호발 부위에 대한 분석)

  • Seoung, Youl-Hun
    • Journal of Digital Convergence
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    • v.10 no.9
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    • pp.391-396
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    • 2012
  • The purpose of this study was to present basic research data to utilize magnetic resonance imaging (MRI) with analyzing intracerebral regional distributions of ischemic cerebrovascular disease of middle aged and oldest-old aged people. We retrospectively analyzed middle-aged group (average age of 44.2 year-old, 43 males, 26 females) and oldest-old aged group (average age of 84.7 year-old, 58 males, 71 females) who taken MRI screening for ischemic cerebrovascular disease from May 2006 year to January 2008 year. The intracerebral vascular were classified into 8 vessels, which anterior communication artery (ACoA), posterior communication artery (PCoA), anterior cerebral artery (ACA), middle cerebral artery (MCA), posterior cerebral artery (PCA), internal carotid artery (ICA), common carotid artery(CCA), and basilar artery (BA). The result of middle-aged group showed that more ischemic cerebrovascular diseases appeared in men than women, and it affected in MCA mostly. In oldest-old aged group, ischemic cerebrovascular diseases occurred evenly spaced in intracerebral region of right, left, and both vessels, and women have more than men. For men, the most occurred in ICA and for women the most occurred in MCA. Specially middle-aged group in men showed that more ischemic cerebrovascular diseases in MCA appeared than oldest-old aged group in men. It is suggested that the analysis on ischemic cerebrovascular could be helpful in the clinical diagnosis and treatment.

A Study on Selection of Optimal Imaging Diagnostic Device for Cerebral Angiography: Focusing on MRA, CTA, and DSA Imaging Diagnosis Devices (뇌혈관 검사 시 최적의 영상 진단장치 선정에 관한 연구: MRA, CTA, DSA, 영상 진단장치 중심으로)

  • Byun, Jung-Su;Goo, Eun-Hoe
    • Journal of the Korean Society of Radiology
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    • v.11 no.7
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    • pp.637-645
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    • 2017
  • The objective of this study was to find the optimum test device for the cerebral blood vessels by comparing and analyzing the SNR and CNR methods for images of three devices (i.e., MRA, CTA, and DSA). The study targeted 90 patients who underwent cerebral angiography from November 2016 to May 2017. The measuring parts were measured by using Rt MCA, Lt MCA, and ACA Image J. The results of quantitative analysis showed that the mean SNR of MRA, the CNR of MRA, the signal strength of MRA, the mean SNR of CTA, the CNR of CTA, the signal strength of CTA, the SNR of DSA, the CNR of DSA, and the signal strength of DSA were evaluated as 254.87, 178.13, 326.81, 74.75, 62.2, 356.66, 26.85, 25.89, and 4400.69, respectively (p<0.05). As a result, both SNR and CNR methods measured it in the order of MRA>CTA>DSA. Statistical significance was determined by using ANOVA analysis at p<0.05 and Bonferroni method was used as a post-hoc analysis SPSS. In conclusion, the results of this study revealed that the optimum imaging devices were MRA, CTA, and DSA after evaluating randomly selected patients with cerebrovascular disease.

Gene Cloning and Expression of Cephalosporin-C Deacetylase from Bacillus sp. KCCM10143

  • Choi, Duk-Ho;Kim, Young-Duk;Chung, Il-Sun;Lee, Sang-Hun;Kang, Sang-Mo;Kwon, Tae-Jon;Han, Kum-Soo
    • Journal of Microbiology and Biotechnology
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    • v.10 no.2
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    • pp.221-226
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    • 2000
  • Cephalosporin-C deacetylase (CAH) catalyzes the deacetylation of cephalosporin derivatives. A novel gene encoding the CAH from Bacillus sp. KCCM10143 was cloned and sepuenced. The uncleotide sequence contained an open reading frame encoding a polypeptide consisting of 217 amino acids and a molecular weight of 24 kDa which was in good agreement with the value obtained by sodium dodecylsulfate-polyacrylamide gel electrophoresis. An expression plasmid was constructed by inserting the CAH gene into the region of the pTrc99A expression vector. An active from of the CAH protein was expressed in the soluble fraction obtained after cell disruption. in fermentation using a 5-1 jar fementer, the transformant E. coli JM109 (pDST654) produced 4.12 U of CAH per ml of culture during 16 h of incubation.

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Clinical Analysis of Stroke in Young Adults (청장년층 뇌졸중에 대한 고찰)

  • 정은정;배형섭;문상관;고창남;조기호;김영석;이경섭
    • The Journal of Korean Medicine
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    • v.21 no.1
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    • pp.84-90
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    • 2000
  • Background and Purpose: Stroke in young adults is relatively uncommon. Only 3.7-14.4% of all strokes occur in patients aged 15-45 years. Stroke in young adults has more various and diverse possible causes than stroke in the elderly. We studied to gain further insight into both pathogenic and etiologic determinants in young adults with stroke. Methods : We retrospectively reviewed the medical records of 230 young patients aged 15-45 years who were admitted to the 2nd internal medicine department of Kyung Hee Oriental Medical Center with a diagnosis of stroke between May 1995 and May 1999. We analysed clinical features and diagnostic tests, such as brain imaging, cerebral angiography, echocardiography, 24 hours holter monitoring and other laboratory tests. Results : 1. Of 230 young patients with stroke aged 15-45 years(176 males(76.5%) and 54 females(23.5%)), 140 patients(60.9%) showed ischemic stroke and 90 patients(39.1 %) showed hemorragic stroke. 2. The most prevalent age group was from 40 to 45 years with 142 patients(61.7%) 3. The most frequent site of 140 ischemic stroke was MCA territory in 93 cases(66.4%) and Multiple, VA territory, PCA territory, ACA territory in order of frequency. 4. The most frequent site of 90 hemorrhagic stroke was basal galglia hemorrhage 57 cases(63.3%) and subcortical 13 cases(14.5%), pons, thalmus, subarachnoid, cerebellum in order of frequency. 5. The causes of hemorrhagic stroke were hypertension 49 cases(54.5%), arteriovenous malformation 7 cases(7.8%), ruptured aneurysm 4 cases(4.5%), angioma 3 cases(3.3%). 6. The risk factors of ischemic stroke were smoking, alcohol drinking, hyperlipidemia, hypertension, obesity, heart disease, history of CVA, diabetes mellitus, in order of frequency. 7. The comparison of risk factors between ischemic and hemorrhagic stroke: hypertension was prevalent in hemorrhagic stroke, heart disease and history of CVA were prevalent in ischemic stroke. Conclusions: From the above results, we found that stroke in young adults had various possible causes. Young adults with stroke deserve an extensive but tailored evaluation which include angiography and echocardiography for diagnosis.

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Analysis of Thin Aggregative Fimbriae Genes csgA, csgB of S. typhimurium and S. enteritidis Strains (S. typhimurium과 S. enteritidis 균주의 Thin Aggregative Fimbriae 유전자 csgA, csgB 분석)

  • Na, Hun-Taek;Joung, Maeng-Sig;Kim, Hong-Seon;Kim, Soo-Young
    • Journal of Naturopathy
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    • v.7 no.1
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    • pp.20-25
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    • 2018
  • The purpose of this study was investigated to observe the relatively low amino acid mutations in six different strains of ATCC or KCTC Salmonella strains (four species and two isolates). The mutations in the strains were to be detected and compared with the genes csgA and csgB corresponding to the Thin aggregative fimbriae. Amino acid mutations in the strains were observed from Ser20→ Gly(AGT→GGT) in the csgA gene, Asp25→Ala(GAT→GCT) and Lys66→Thr(AAA→ACA) in the csgB gene. Among the six strains, the two most common amino acid variations were observed in S. typhimurium - TH strains. On the other hand, no mutation of nucleotide sequence was observed in the strains of S. typhimurium ATCC 13311 and S. typhimurium KCTC 1925. In conclusion the genes csgA and csgB in the strains may be useful for the evaluation and detection of amino acid mutation.

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