Search: id:"swepub:oai:DiVA.org:su-35094" >
Synthesis and SAR o...
Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease : exploration of P2 quinazoline substituents.
-
Nilsson, Magnus (author)
-
Belfrage, Anna Karin (author)
-
Lindström, Stefan (author)
-
show more...
-
Wähling, Horst (author)
-
- Lindquist, Charlotta (author)
- Stockholms universitet,Institutionen för organisk kemi
-
Ayesa Alvarez, Susana (author)
-
Kahnberg, Pia (author)
-
Pelcman, Mikael (author)
-
Vrang, Lotta (author)
-
Terselius, Ylva (author)
-
Wikström, Kristina (author)
-
Hamelink, Elizabeth (author)
-
Rydergård, Christina (author)
-
Edlund, Michael (author)
-
Eneroth, Anders (author)
-
Raboisson, Pierre (author)
-
Lin, Tse-I. (author)
-
de Kock, Herman (author)
-
Wigerinck, Piet (author)
-
Simmen, Kenneth (author)
-
Samuelsson, Bertil (author)
-
Rosenquist, Åsa (author)
-
show less...
-
(creator_code:org_t)
- English.
- Related links:
-
https://urn.kb.se/re...
Abstract
Subject headings
Close
- Novel NS3/4A protease inhibitors comprising quinazoline derivatives as P2 substituent were synthesized. High potency inhibitors displaying advantageous PK properties have been obtained through the optimization of quinazoline P2 substituents in three series of macrocyclic P2 cyclopentane dicarboxylic acid and P2 proline urea motifs. For the quinazoline moiety it was found that 8-methyl substitution for the P2 cyclopentane dicarboxylic acid series improved on the stability in human liver microsomes. By comparison, the proline urea series displayed advantageous Caco-2 permeability over the cyclopentane series. properties were assessed in rat on selected compounds. Excellent exposure and liver–to-plasma ratios were demonstrated for a member of the 14-membered quinazoline substituted P2 proline urea series. In vivo pharmacokinetic properties were assessed in rat on selected compounds. Excellent exposure and liver–to-plasma ratios were demonstrated for a member of the 14-membered quinazoline substituted P2 proline urea series.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- Pharmaceutical chemistry
- Läkemedelskemi
- organisk kemi
- Organic Chemistry
Publication and Content Type
- vet (subject category)
- ovr (subject category)
To the university's database
- By the author/editor
-
Nilsson, Magnus
-
Belfrage, Anna K ...
-
Lindström, Stefa ...
-
Wähling, Horst
-
Lindquist, Charl ...
-
Ayesa Alvarez, S ...
-
show more...
-
Kahnberg, Pia
-
Pelcman, Mikael
-
Vrang, Lotta
-
Terselius, Ylva
-
Wikström, Kristi ...
-
Hamelink, Elizab ...
-
Rydergård, Chris ...
-
Edlund, Michael
-
Eneroth, Anders
-
Raboisson, Pierr ...
-
Lin, Tse-I.
-
de Kock, Herman
-
Wigerinck, Piet
-
Simmen, Kenneth
-
Samuelsson, Bert ...
-
Rosenquist, Åsa
-
show less...
- About the subject
-
- MEDICAL AND HEALTH SCIENCES
-
MEDICAL AND HEAL ...
-
and Basic Medicine
-
and Medicinal Chemis ...
- By the university
-
Stockholm University