New inhibitors of the malaria aspartyl proteases plasmepsin I and II
2003 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, Vol. 11, no 16, 3423-3437 p.Article in journal (Refereed) Published
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.
Engineering and Technology
IdentifiersURN: urn:nbn:se:liu:diva-46526DOI: 10.1016/S0968-0896(03)00312-2OAI: oai:DiVA.org:liu-46526DiVA: diva2:267422