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Activity of natural and synthetic polygodial derivatives against Trypanosoma cruzi amastigotes, trypomastigotes and epimastigotes

journal contribution
posted on 2023-05-20, 05:49 authored by Turner, DN, Just, J, Dasari, R, Jason SmithJason Smith, Alexander BissemberAlexander Bissember, Kornienko, A, Rogelj, S
Our laboratories have been investigating biological effects of a sesquiterpenoid polygodial and its natural and synthetic analogues. Herein, we report the evaluation of these compounds against the three forms of Trypanosoma cruzi, amastigotes, trypomastigotes and epimastigotes. Although polygodial was found to be poorly active, its natural congener epipolygodial and synthetic Wittig-derived analogues showed low micromolar potency against all three forms of the parasite. Synthetic α,β-unsaturated phosphonate 9 compared favorably with clinically approved drugs benznidazole and nifurtimox, and was effective against trypomastigotes, toward which benznidazole showed no activity.

History

Publication title

Natural Product Research

Volume

35

Issue

5

Pagination

792-795

ISSN

1478-6419

Department/School

Tasmanian Institute of Agriculture (TIA)

Publisher

Taylor & Francis Ltd

Place of publication

Abingdon, England

Rights statement

Copyright 2019 Informa UK Limited, trading as Taylor & Francis Group

Repository Status

  • Restricted

Socio-economic Objectives

Expanding knowledge in the chemical sciences

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