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Design and Synthesi...
Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors Incorporating a P2 Cyclopentane-Derived Scaffold
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- Bäck, Marcus, 1979- (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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- Sandström, Anja, Dr. (opponent)
- Department of Medicinal Chemistry Organic, Pharmaceutical Chemistry, BMC Uppsala
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(creator_code:org_t)
- ISBN 9185523208
- Institutionen för fysik, kemi och biologi, 2006
- English 40 s.
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Series: Linköping Studies in Science and Technology. Thesis, 0280-7971 ; 1265
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Abstract
Subject headings
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- 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.
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
Keyword
- HCV
- NS3 protease
- Proline mimic
- Cyclopentane-derived scaffold
- Linear inhibitors
- Macrocyclic inhibitors
- Organic synthesis
- Organisk syntes
Publication and Content Type
- vet (subject category)
- lic (subject category)
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