95 resultados para Lipase EC 3.1.1.3
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一种新型的2,4-二取代氨基-6-取代-[1,3,5]三嗪或1,3-嘧啶衍生物及其制备方法、药物组合物和其药理用途,其结构通式如式(I)所示,其中R1、R2、R3、R4、R5、R6、A、B、X、Y和Z的定义如说明书中所述。该类化合物与HIV-1整合酶具有很高结合活性,并且在底物竞争测试中能够有效的抑制整合酶对底物的结合。因此该类化合物是较强的HIV-1整合酶抑制剂,有望开发成为新的抗HIV病毒药物。
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In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a-1) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds
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In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC50 values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs. (C) 2010 Elsevier Ltd. All rights reserved.
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Nostoc sphaeroides Kutzing was cultivated in paddlewheel-driven raceway ponds and the growth kinetics of 1-2 mm and 3-4 mm colonies of N. sphaeroides was studied. The biomass productivities in 2.5 m(2) raceway ponds inoculated with 1-2 mm and 3-4 mm colonies were 5.2 and 0.25 g dry wt m(-2) stop d(-1), respectively. Furthermore, differently sized colonies showed different relative water content, total soluble carbohydrates, chlorophyll a content and density of filaments. This is the first report on mass culture of N. sphaeroides under outdoor conditions.
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The genome segments 1, 2, and 3 of the grass carp reovirus (GCRV), a tentative species assigned to genus Aquareouirus, family Reouiridae, were sequenced. The respective segments 1, 2, and 3 were 3949, 3877, and 3702 nucleotides long. Conserved moths 5' (GUUAUUU) and 3' (UUCAUC) were found at the ends of each segment. Each segment contains a single ORF and the negative strand does not permit identification of consistent ORFs. Sequence analysis revealed that VP2 is the viral polymerase, while VPI might represent the viral guanyly/methyl transferase (involved in the capping process of RNA transcripts) and VP3 the NTPase/helicase (involved in the transcription and capping of viral RNAs), The highest amino acid identities (26-41%) were found with orthoreovirus proteins. Further genomic characterization should provide insight about the genetic relationships between GCRV, aquareoviruses, and orthoreoviruses, It should also permit to precise the taxonomic status of these different viruses. (C) 2000 Academic Press.
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z
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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z