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pubmed:abstractText |
A series of malaria plasmepsin (Plm) I and II inhibitors containing a C(2)-symmetric core structure have been synthesised and tested for protease inhibition activity. These compounds can be prepared using a straightforward synthesis involving a phenol nucleophilic ring opening of a diepoxide. Exemplar compounds synthesised exhibited remarkable inhibitory activity against both Plm I and II, notably 15c with K(i) values of 2.7nM and 0.25nM respectively, as well as showing >100-fold selectivity against Cathepsin D.
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pubmed:affiliation |
Department of Organic Chemistry, Arrhenius Laboratory, Floor 6, Stockholm University, S-106 91, Stockholm, Sweden. bertil.samuelsson@medivir.se
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