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High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
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2003 (English)In: Journal of combinatorial chemistry, ISSN 1520-4766, E-ISSN 1520-4774, Vol. 5, no 4, 456-464 p.Article in journal (Refereed) Published
Abstract [en]

Four focused libraries targeted for inhibition of the malarial proteases plasmepsin I and II were designed, synthesized, purified, and screened. Selected carboxylic acids and organometallic reactants with diverse physical properties were attached to the hydroxylethylamine scaffold in the P3 and P1‘ positions to furnish inhibitors with highly improved activity. The concept of controlled and sequential microwave heating was employed for rapid library generation. This combinatorial optimization protocol afforded plasmepsin inhibitors not only with Ki values in the low nanomolar range, but also with high selectivity versus the human protease cathepsin D. With this class of inhibitory agents, modifications of the P1‘ substituents resulted in the largest impact on the plasmepsin/cathepsin D selectivity.

Place, publisher, year, edition, pages
2003. Vol. 5, no 4, 456-464 p.
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Medicinal Chemistry
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URN: urn:nbn:se:uu:diva-66052DOI: 10.1021/cc0301014PubMedID: 12857114OAI: oai:DiVA.org:uu-66052DiVA: diva2:93963
Available from: 2008-10-17 Created: 2008-10-17 Last updated: 2017-11-28Bibliographically approved

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Schaal, WesleyLarhed, Mats

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