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Finasteride has been facilely synthesized from 4-androstene-3, 17-dione by oxidation, ammoniumation, cyanohydrin, dehydration, Ritter reaction, hydrogenation and dehydrogenation.

本文参考有关文献,以雄烯二酮为起始原料,经氧化开环、内酰胺化、氰醇化、Ritter反应引入叔丁基酰胺、氢化还原、最后氧化脱氢制得非那雄胺。

Results: The proportion of Gram-negative bacilli rose obviously, so did the opportunistic pathogen's and Yeasts detected rate. Most drug sensitive tests showed the drug-fast rate turned to be high. Escherichia coli, Salmonella and Citrobacter resistant and so on to fluoroquinolones was 57%~97%. These bacteria to imipenem showed excellent activity. Meticillin-resistant-staphylococcus resistant to ciprofloxacin, norfloxacin, clindamycin, tetracycline, erythromycin, cefazolin and ampicillin were 40.9%, 42.4%, 63.6%, 72.2%, 85.9%, 100.0% and 100.0%, respectively Streptococcus and Enterococcus resistant to major β-lactams-penicillin, aminoglycosides, macrolides, tetracyclines and sulfonamides were between 36.0% to 100.0%.

结果:革兰阴性杆菌比例显著升高,条件致病菌和酵母样真菌检出机会显著增多;药敏结果显示多数临床细菌对常用抗生素的耐药趋势在不断上升;大肠埃希菌、沙门菌和枸橼酸杆菌等革兰阴性杆菌对喹诺酮类药物的耐药率达57%~97%,亚胺培南则对阴性杆菌有较高的敏感覆盖率;耐甲氧西林葡萄球菌对环丙沙星、诺氟沙星、氯洁霉素、四环素、红霉素、头孢唑啉和氨苄西林的耐药率分别为40.9%、42.4%、63.6%、70.2%、85.9%、100.0%和100.0%;链球菌和肠球菌对多数β内酰胺类青霉素、氨基糖苷类、大环内酯类、四环素类以及磺胺类药物均呈高度耐药,耐药率在36%~100%。

To Dec. 2003 years in Yuxi city People's Hospital. RESULTS: The proportion of G- bacilli were much. The opportunistic pathogen's and Yeasts detected rate rose obviously. Most drug sensitive tests showed the drug-fast rate turned to be high. Escherichia coli, Salmonella and Klebsiella and so on to fluoroquinolones was 50~97.7%. These bacteria to imipenem showed excellent activity. MRS resistant to ciprofloxacin, norfloxacin, clindamycin, tetracycline, erythromycin, gentamycin, trimeth/sulfa and cefazolin were above 50%. Streptococcus resistant to major β-lactams-penicillin, aminoglycosides, macrolides, tetracyclines and sulfonomides were highness.

结果:G-杆菌比例居多,条件致病菌和酵母样真菌检出机会显著增高;药敏结果显示多数临床细菌对常用抗生素的耐药趋势在不断上升;大肠埃希菌、沙门菌和克雷伯菌等G-杆菌对喹诺酮类药物的耐药率在50%~97.7%,亚胺培南则对阴性杆菌有较高的敏感覆盖率;耐甲氧西林葡萄球菌对环丙沙星、诺氟沙星、氯洁霉素、四环素、红霉素、庆大霉素、复方新诺明和头孢唑啉的耐药率均在50%以上,链球菌对多数β内酰胺类青霉素、氨基糖苷类、大环内酯类、四环素类以及磺胺类药物呈高度耐药。

Low-valent titanium reagent induced the monomolecular reduction of N-substitutedphthalimides supplied a new method of synthesis hydroxyl lactams. This method was moreeconomic, convenient and in higher yields comparing with other methods reported before,therefore it has practical value.

4低价钛试剂引起邻苯二甲酰亚胺的单分子还原反应提供了一种合成羟基内酰胺的新方法,和文献方法相比,我们的方法试剂便宜易得,毋需溶剂,操作简便,收率也有所提高,具有实用价值。

Arkema has developed this kind of polyamide powders for their solvent and heat resistance as well as their hardness.

代表一个系列的超细聚酰胺粉末,它是由十二内酰胺和/或己内酰胺聚合而得到。

Results After screening, 59 subtracted library clones were isolated which were specific for strain VIB72, and the DNA sequences of these clones were determined. Seventeen fragments showed high homology to the genes of known functions in other bacteria. This includes soluble lytic murein transglycosylase, mobilization protein, transposase (IS66), resistance-related protein (metallo-beta-lactamase and acetyltransferase family), toxin protein (DT-201 and alveicin A immunity protein), ATP-dependent endonuclease of OLD family like protein, SocE and GTP-binding protein HflX (high frequency of lysogenization).

通过对差减文库筛选,分离到59个对菌株VIB72的克隆,并对这些克隆的DNA序列进行了测定。17个基因片断与其它细菌的已知功能的基因有较高的同源性,其中包括可溶性溶胞壁质转糖基酶、转移蛋白MobA和MobC、转座子IS66、抑制相关蛋白(金属β-内酰胺酶和乙酰转移酶家族)、毒素蛋白(DT-201和alveicin A免疫蛋白)、与OLD 家族相似的ATP依赖性核酸内切酶以及SocE 和GTP结合蛋白HflX。

Objective To investigate extended-spectrumβ-lactamasesand AmpCβ-lactamases and metalloβ-lactamasesproducing by gram-negative bacilli in burns.Mehtods Adopitng double-disk synergy test,modified three-dimensional extract test and the enzyme inhibitor of EDTA-Na2to detect ESBLs and AmpC and mBLA producing strains.

目的 了解烧伤感染主要革兰阴性杆菌产超广谱β-内酰胺酶、AmpC酶和金属β-内酰胺酶及其对常用抗生素耐药性情况,指导烧伤医院感染合理用药。

Objective To investigate extended-spectrumβ-lactamasesand AmpCβ-lactamases and metalloβ-lactamasesproducing by gram-negative bacilli in burns.Mehtods Adopitng double-disk synergy test,modified three-dimensional extract test and the enzyme inhibitor of EDTA-Na2to detect ESBLs and AmpC and mBLA producing strains.Using K-B test to perform the susceptibility testing.Results Among348strains of gram negative bacilli,ESBLs,AmpCβ-lactamases,ESBLs combined with ApmCβ-lactamases and mBLA produc-ing strains were found in122,47,9and20strains,the incidence being35.1%,13.5%,2.6%and5.7%respec-tively.

目的 了解烧伤感染主要革兰阴性杆菌产超广谱β-内酰胺酶、AmpC酶和金属β-内酰胺酶及其对常用抗生素耐药性情况,指导烧伤医院感染合理用药方法采用双纸片协同试验检测产ESBLs株,头孢西丁三维试验检测产AmpC酶株,头孢曲松三维试验检测同时产ESBLs和AmpC酶株,依地酸二钠协同试验检测产mBLA株,K-B法进行G -杆菌药敏试验。

A plausible process of this reaction is as following: Aldehyde was in equilibrium with the enol form, aldehyde reacted with aniline catalyzed by 2,2,2-trichloroacetic acid to afford imine, the generated imine immediately reacted with enol to form intermediate via intramolecular cyclization.

我们发现一分子芳基叠氮和一分子三苯基磷反应生成一分子磷亚胺,后者与由两分子取代的苯氧乙酰氯原位生成的烯酮反应生成4-亚烷基-β-烷基-内酰胺,其串联过程涉及烯酮亚胺的形成及其与烯酮的[2+2]的环加成反应。

When the platform of screening β-lactamse inhibitor is constructed,it can not only be used to find new compounds for treating bacteria which resist β-lactam antibiotics, but also be used to screen inhibitors of hydrolase or modifying enzyme which is related to drug resistent bateria.

通过建立β-内酰胺酶抑制剂筛选的平台,不仅为寻找治疗β-内酰胺类抗生素耐药菌开辟一条新途径,并且这一新方法也适用于筛选与细菌耐药有关的其它一些由细菌产生的水解或修饰酶的抑制剂。

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