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J Med Chem. 2014 Dec 26;57(24):10557-63. doi: 10.1021/jm501439w. Epub 2014 Dec 8.

Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.

Author information

1
School of Chemistry, The University of Sydney , Building F11, Sydney, New South Wales 2006, Australia.

Abstract

Analogues of the natural product gallinamide A were prepared to elucidate novel inhibitors of the falcipain cysteine proteases. Analogues exhibited potent inhibition of falcipain-2 (FP-2) and falcipain-3 (FP-3) and of the development of Plasmodium falciparum in vitro. Several compounds were equipotent to chloroquine as inhibitors of the 3D7 strain of P. falciparum and maintained potent activity against the chloroquine-resistant Dd2 parasite. These compounds serve as promising leads for the development of novel antimalarial agents.

PMID:
25412465
DOI:
10.1021/jm501439w
[Indexed for MEDLINE]

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