Search: onr:"swepub:oai:DiVA.org:liu-46526" >
New inhibitors of t...
New inhibitors of the malaria aspartyl proteases plasmepsin I and II
-
- Dahlgren, Anders (author)
- Linköpings universitet,Tekniska högskolan,Organisk Kemi
-
- Kvarnström, Ingemar (author)
- Linköpings universitet,Tekniska högskolan,Organisk Kemi
-
- Vrang, L. (author)
- Medivir AB, Lunastigen 7, S-141 44 Huddinge, Sweden
-
show more...
-
- Hamelink, E. (author)
- Medivir AB, Lunastigen 7, S-141 44 Huddinge, Sweden
-
- Hallberg, A. (author)
- Dept. of Organ. Pharmaceutical Chem., BMC, Uppsala University, S-751 24 Uppsala, Sweden
-
Rosenquist, A. (author)
-
- Samuelsson, B. (author)
- Medivir AB, Lunastigen 7, S-141 44 Huddinge, Sweden, Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, S-106 91 Stockholm, Sweden
-
show less...
-
(creator_code:org_t)
- 2003
- 2003
- English.
-
In: Bioorganic & Medicinal Chemistry. - 0968-0896 .- 1464-3391. ; 11:16, s. 3423-3437
- Related links:
-
https://urn.kb.se/re...
-
show more...
-
https://doi.org/10.1...
-
show less...
Abstract
Subject headings
Close
- New inhibitors of plasmepsin I and II, the aspartic proteases of the malaria parasite Plasmodium falciparum, are described. From paralell solution phase chemistry, several reversed-statine type isostere inhibitors, many of which are aza-peptides, have been prepared. The synthetic strategy delivers the target compounds in good to high overall yields and with excellent stereochemical control throughout the developed route. The final products were tested for their plasmepsin I and II inhibiting properties and were found to exhibit modest but promising activity. The best inhibitor exhibits Ki values of 250 nM and 1.4 µM for Plm I and II, respectively. © 2003 Elsevier Ltd. All rights reserved.
Keyword
- TECHNOLOGY
- TEKNIKVETENSKAP
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
To the university's database