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N-(5-氯-8-羟基-2-苯乙烯基喹啉-7-基)苯磺酰胺衍生物的设计、合成及抗 HIV 整合酶活性评价。

Design, synthesis and anti-HIV integrase evaluation of N-(5-chloro-8-hydroxy-2-styrylquinolin-7-yl)benzenesulfonamide derivatives.

机构信息

College of Life Science & Bioengineering, Beijing University of Technology, Beijing, China.

出版信息

Molecules. 2010 Mar 16;15(3):1903-17. doi: 10.3390/molecules15031903.

Abstract

Styrylquinoline derivatives are demonstrated to be HIV-1 integrase inhibitors. On the basis of our previous CoMFA analysis of a series of styrylquinoline derivatives, N-[(2-substituted-styryl)-5-chloro-8-hydroxyquinolin-7-yl]-benzenesulfonamide derivatives were designed and synthesized,and their possible HIV IN inhibitory activity was evaluated.

摘要

苯乙烯基喹啉衍生物被证实为 HIV-1 整合酶抑制剂。基于我们之前对一系列苯乙烯基喹啉衍生物的 CoMFA 分析,设计并合成了 N-[(2-取代苯乙烯基)-5-氯-8-羟基喹啉-7-基]-苯磺酰胺衍生物,并评估了它们可能的 HIV IN 抑制活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf9d/6257356/28769884cc33/molecules-15-01903-g001.jpg

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本文引用的文献

1
Derivatives of 5-chloro-8-hydroxyquinoline.
J Am Chem Soc. 1947 May;69(5):1222. doi: 10.1021/ja01197a516.
2
A novel high-throughput format assay for HIV-1 integrase strand transfer reaction using magnetic beads.
Acta Pharmacol Sin. 2008 Mar;29(3):397-404. doi: 10.1111/j.1745-7254.2008.00748.x.
4
Synthesis of analogues of Congo red and evaluation of their anti-prion activity.
J Med Chem. 2004 Oct 21;47(22):5515-34. doi: 10.1021/jm049922t.
6
Automation in medicinal chemistry.
Curr Top Med Chem. 2004;4(7):671-86. doi: 10.2174/1568026043451069.
7
Synthesis of styrylbenzofuran derivatives as styrylquinoline analogues for HIV-1 integrase inhibitor.
Farmaco. 2003 Dec;58(12):1243-50. doi: 10.1016/j.farmac.2003.08.001.
9
In search of authentic inhibitors of HIV-1 integration.
Antivir Chem Chemother. 2002 Jan;13(1):1-15. doi: 10.1177/095632020201300101.
10
Strategies in the design of antiviral drugs.
Nat Rev Drug Discov. 2002 Jan;1(1):13-25. doi: 10.1038/nrd703.

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