Synthesis of gallinamide a analogues as potent falcipain inhibitors and antimalarials

Trent Conroy, Jin T Guo, Nabiha Elias, Katie M Cergol, Jiri Gut, Jennifer Legac, Lubna Khatoon, Yang Liu, Sheena McGowan, Philip J Rosenthal, Nicholas Henry Hunt, Richard J Payne

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)10557 - 10563
Number of pages7
JournalJournal of Medicinal Chemistry
Volume57
Issue number24
DOIs
Publication statusPublished - 2014

Cite this