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To detect the marks reflecting the liver functions as follows:①The marks to reflect the capability to synthesize proteins, TPROT, ALB, GLB;②The marks to reflect the injury of the liver cells: AST, ALT, CHE;③The marks to reflect the capability to egest the bile, excrect, and detoxicate: TBILI, DBILI, IBILI, TBA;④The enzymes to reflect the cholestasis: GGT, ALP. Results The results of both the morphological and the pathological studies showed that the degree of the liver cirrhosis was of the terminal stage.

肝功能指标:①反映肝细胞蛋白合成代谢功能的指标:总蛋白TPROT,白蛋白ALB,球蛋白GLB;②肝细胞受损的指标;谷草转氨酶AST,谷丙转氨酶ALT,胆碱脂酶CHE;③反映肝脏胆排泄、分泌及解毒功能的指标:总胆红素TBILI,直接胆红素DBILI,间接胆红素IBILI,总胆汁酸TBA;④胆汁淤积指示酶:谷氨酰转肽酶GGT,碱性磷酸酶ALP。

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%。

In Studies 1–3,the antinociceptive and antiinflammatory effects of IM ketorolactromethamine and its base and propyl ester were evaluated.

在研究1-3中,评估了 IM 酮咯酸氨丁三醇和它的原制剂和丙基酯的抗伤害和抗炎效应。

During these years (1997-2000) in the research area of annonaceous acetogenins 5 natural products and a number of chiral-pure analogs of annonaceous acetogenins have been synthesized using sugars as the starting materials. Their high activity and selectivity against cell line of colon tumor and a relationship between activity and configuration have been found too. In the respect of inhibitor of sialidase two new methodologies for the synthesis of chiral-pure 3-deoxy-ulosonic acid using hetero-Diels-Alder reaction or asymmetric propargylation as the key reaction were developed. On the topic of anti-leukemia marine natural product clavulactone a synthetic method based on the free radical cyclization and starting from sugar has been developed. In other title of PKC inhibited agent sphingosine a new synthetic route with SN2' as the key reaction has also been disclosed.

项目期间(1997-2000)在番荔枝内酯方面从糖出发合成了五个天然产物和一批手性纯的类似物,它们对肠癌细胞有很高的活性和选择性,并与构型有关;在唾液酸酶抑制剂方面发展了二类全新手性纯高碳糖的合成方法-杂原子D-A反应或丙炔基不对称加成为关键的反应;抗白血病海洋天然产物群柱虫内酯方面研究了由糖出发和自由基环化反应的合成方法;对PKC 起抑制作用的鞘氨醇方面也开创了新的合成途径-由糖出发并以SN2'反应为关键反应。

The formation of charge transfer complex was studied in the first part. The second part includes the synthesis and characterization of the acrylated unsaturated polyester and the kinetic studies on the Ar-UPE/ triethylene divinyl ether (DVE-3) photocuring system, the rheology and properties of film after photocuring. The third part includes the synthesis and characterization of the urethane modified unsaturated polyester and the kinetic studies on the PU-UPE/DVE-3 photocuring system, the rheology and properties of film after photocuring. The fourth part includes the synthesis and characterization of the vinyl ether end capped polyurethane and the kinetic studies on the VE-PU/DVE3 photocuring system, the rheology and properties of film after photocuring.

整个研究工作分为四个部分:一是电荷转移复合物的研究;二是丙烯酰氧基化不饱和聚酯的合成,表征,Ar-UPE/二缩乙二醇二乙烯基醚(DVE-3)体系光固化动力学研究以及Ar-UPE/DVE-3体系流变性能和光固化后涂膜综合性能的研究;三是氨酯改性的不饱和聚酯的合成,表征,PU-UPE/DVE-3体系光固化动力学研究以及该体系光固化后涂膜综合性能的研究;四是乙烯基醚封端的聚氨酯的合成,表征,VE-PU/马来酸二甲酯体系光固化动力学研究以及VE-PU/DMA体系流变性能和光固化后涂膜综合性能的研究。

Bezaldehyde was used as protective agent in first method.S-Epichloeohydrin was aminated and acidulated to give(2S)-1-Amino-3-chloro-propanol Salts.The acetylation of (2S)-1-Amino-3-chloro-propanol by acetic anhydride produced the intermediate-N-[2--3-chloropropyl]acetamide.And then at 20℃,in the presence of lithium tert-butoxide,benzyl 3-fluoro-4-morpholinophenyl carbamate react with-N-[2--3-chloropropyl]acetamide to give linezolid in total yield of 43.6%.

路线一采用苯甲醛作保护剂,使S-环氧氯丙烷氨解、酸化生成S-1-氨基-3-氯-2-丙醇盐酸盐,然后经乙酰化反应后,生成中间体-N-[2-乙酰氧基-3-氯丙基]乙酰胺,再用N-(3-氟-4-吗啉苯基)氨基甲酸苄酯和中间体在催化剂叔丁醇锂存在下25℃反应生成利奈唑酮,总产率达到43.6%。

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