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Potent Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease. Use of Cyclopentane and Cyclopentene Derived P2-Scaffolds
Linköping University, The Department of Physics, Chemistry and Biology.
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Manuscript (Other academic)
Identifiers
URN: urn:nbn:se:liu:diva-14309OAI: oai:DiVA.org:liu-14309DiVA: diva2:23196
Available from: 2007-02-21 Created: 2007-02-21 Last updated: 2010-01-13
In thesis
1. Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors Incorporating a P2 Cyclopentane-Derived Scaffold
Open this publication in new window or tab >>Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors Incorporating a P2 Cyclopentane-Derived Scaffold
2006 (English)Licentiate thesis, comprehensive summary (Other academic)
Abstract [en]

This thesis describes the design, synthesis and structure-activity relationships analysis of potential inhibitors targeting the hepatitis C virus (HCV) NS3 protease. Also discussed is the disease caused by HCV infection and the class of enzymes known as proteases. Furthermore are explained why such enzymes can be considered to be suitable targets for developing drugs to combat diseases in general and in particular HCV, focusing on the NS3 protease. Moreover, some strategies used to design protease inhibitors and the desired properties of potential drug candidates are briefly examined. Synthesis of linear and macrocyclic NS3 protease inhibitors comprising a designed trisubstituted cyclopentane moiety as an N-acyl-(4R)-hydroxyproline bioisostere is also addressed, and several very potent and promising compounds are evaluated.

Place, publisher, year, edition, pages
Institutionen för fysik, kemi och biologi, 2006. 40 p.
Series
Linköping Studies in Science and Technology. Thesis, ISSN 0280-7971 ; 1265
Keyword
HCV, NS3 protease, Proline mimic, Cyclopentane-derived scaffold, Linear inhibitors, Macrocyclic inhibitors
National Category
Organic Chemistry
Identifiers
urn:nbn:se:liu:diva-8395 (URN)91-85523-20-8 (ISBN)
Presentation
2006-09-26, Schrödinger, Fysikhuset, Campus Valla, Linköpings universitet, Linköping, 00:00 (English)
Opponent
Note
Report code: LIU-TEK-LIC-2006:46.Available from: 2007-02-21 Created: 2007-02-21 Last updated: 2009-03-02

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Total: 40 hits
CiteExportLink to record
Permanent link

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Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • oxford
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf