Synthesis of Gallinamide A Analogues as Potent Falcipain Inhibitors and Antimalarials | Zendy

Trent Conroy | Zendy; Jintao Guo | Zendy; Nabiha Elias | Zendy; Katie M. Cergol | Zendy; Jiří Gut | Zendy; Jennifer Legac | Zendy; Lubna Khatoon | Zendy; Yang Liu | Zendy; Sheena McGowan | Zendy; Philip J. Rosenthal | Zendy; Nicholas H. Hunt | Zendy; Richard J. Payne | Zendy

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Synthesis of Gallinamide A Analogues as Potent Falcipain Inhibitors and Antimalarials

Author(s) -

Trent Conroy,

Jintao Guo,

Nabiha Elias,

Katie M. Cergol,

Jiří Gut,

Jennifer Legac,

Lubna Khatoon,

Yang Liu,

Sheena McGowan,

Philip J. Rosenthal,

Nicholas H. Hunt,

Richard J. Payne

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm501439w

Subject(s) - plasmodium falciparum , chemistry , natural product , chloroquine , proteases , in vitro , cysteine protease , enzyme , stereochemistry , enzyme inhibitor , structure–activity relationship , biochemistry , malaria , biology , immunology

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.

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