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Solid-phase library synthesis of reversed-statine type inhibitors of the malarial 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 6, 827-841 p.Article in journal (Refereed) Published
Abstract [en]

With the aim to develop inhibitors of the plasmepsin I and II aspartic proteases of the malaria parasite Plasmodium falciparum, we have synthesized sets of libraries from novel reversed-statine isosteres, using a combination of solution phase and solid phase chemistry. The synthetic strategy furnishes the library compounds in good to high overall yields and with excellent stereochemical control throughout the developed route. The products were evaluated for their plasmepsin I and II inhibiting properties and were found to exhibit modest but promising activity. The best inhibitor exhibits an in vitro activity of 28% inhibition of plasmepsin II at an inhibitor concentration of 0.5 µM (Ki for Plm II=5.4 µM). © 2003 Elsevier Science Ltd. All rights reserved.

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2003. Vol. 11, no 6, 827-841 p.
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Engineering and Technology
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URN: urn:nbn:se:liu:diva-46636DOI: 10.1016/S0968-0896(02)00568-0OAI: oai:DiVA.org:liu-46636DiVA: diva2:267532
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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