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L-样5'-去氧阿瑞吡坦的N-6取代脱氧衍生物

N-6 Substituted Deoxygenated Derivatives of L-like 5'-Noraristeromycin.

作者信息

Yu Henry, Serbessa Tesfaye

机构信息

Elizabeth City State University, Department of Chemistry, Geology, and Physics Elizabeth city, NC 27909 USA.

出版信息

Bull Chem Soc Ethiop. 2010;24(3):439-446. doi: 10.4314/bcse.v24i3.60692.

DOI:10.4314/bcse.v24i3.60692
PMID:21822360
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3149869/
Abstract

Several N-6 substituted derivatives (4-11) of (+)-4'-deoxy-5'-noraristeromycin (2) and its unsaturated counterpart (3) have been prepared. The derivatives are designed to systematically vary the hydrophobic/hydrophilic balance of the lead compounds. These compounds were evaluated against a large number of viruses but, no significant antiviral activity was observed. Also, no cytotoxicity to host cells was found.

摘要

已制备了几种(+)-4'-脱氧-5'-去甲阿瑞司他霉素(2)及其不饱和类似物(3)的N-6取代衍生物(4-11)。设计这些衍生物是为了系统地改变先导化合物的疏水/亲水平衡。对这些化合物针对大量病毒进行了评估,但未观察到明显的抗病毒活性。此外,未发现对宿主细胞的细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/0560f72a4c22/nihms251158f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/f4c344b871eb/nihms251158f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/6c7f214b1357/nihms251158f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/3cfef0dff8fa/nihms251158f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/16f1a2819765/nihms251158f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/0560f72a4c22/nihms251158f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/f4c344b871eb/nihms251158f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/6c7f214b1357/nihms251158f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/3cfef0dff8fa/nihms251158f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/16f1a2819765/nihms251158f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/022b/3149869/0560f72a4c22/nihms251158f5.jpg

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J Med Chem. 1998 Jun 4;41(12):2168-70. doi: 10.1021/jm980038a.
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Synthesis and antitrypanosomal activities of a series of 7-deaza-5'-noraristeromycin derivatives with variations in the cyclopentyl ring substituents.一系列环戊基环取代基有变化的7-脱氮-5'-去甲阿瑞吡坦霉素衍生物的合成及抗锥虫活性
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