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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, SOur 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 ResearchVolume
35Issue
5Pagination
792-795ISSN
1478-6419Department/School
Tasmanian Institute of Agriculture (TIA)Publisher
Taylor & Francis LtdPlace of publication
Abingdon, EnglandRights statement
Copyright 2019 Informa UK Limited, trading as Taylor & Francis GroupRepository Status
- Restricted