Journal
CHEMISTRY & BIODIVERSITY
Volume 14, Issue 8, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201700037
Keywords
Antimalarial activities; Peptidomimetics; Falcipain; Drug design; Synthesis
Funding
- CDC Cooperative Agreement [UR3/CCU4186520-03]
- University of Mississippi, MS, USA
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A new series of peptidomimetic N-substituted Cbz-4-Hyp-Hpa-amides were designed, synthesized, and evaluated for inhibition of the Plasmodium falciparum. Substituents on the N-atom of the amide group were selected alkyl-, allyl-, aryl-, 2-hydroxyethyl-, 2-cyanoethyl-, cyanomethyl-, 2-hydroxyethyl-, 2,2-diethoxyethyl-, or 2-ethoxy-2-oxoethylamino groups, and about of 40 new compounds were synthesized and evaluated for antiplasmodial activity invitro. Antimalarial activity has been investigated as for the final peptide mimetics, and their immediate predecessors, carrying TBDMS or TBDPS protecting groups on 4-hydroxyproline residue and 18 derivatives exhibited toxicity against P.falciparum. Of these agents, compound 23e was shown to have potent antimalarial activity with IC50 528ng/ml.
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