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New inhibitors of the malaria aspartyl proteases plasmepsin I and II
Linköping University, The Institute of Technology. Linköping University, Department of Physics, Chemistry and Biology, Organic Chemistry .
Linköping University, The Institute of Technology. Linköping University, Department of Physics, Chemistry and Biology, Organic Chemistry .
Medivir AB, Lunastigen 7, S-141 44 Huddinge, Sweden.
Medivir AB, Lunastigen 7, S-141 44 Huddinge, Sweden.
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2003 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 11, no 16, 3423-3437 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2003. Vol. 11, no 16, 3423-3437 p.
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Engineering and Technology
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URN: urn:nbn:se:liu:diva-46526DOI: 10.1016/S0968-0896(03)00312-2OAI: oai:DiVA.org:liu-46526DiVA: diva2:267422
Available from: 2009-10-11 Created: 2009-10-11 Last updated: 2017-12-13

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Dahlgren, AndersKvarnström, Ingemar

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