Tropical Medicine Center, Faculty of Medicine, University of Brasília, Campus Universitário Darcy Ribeiro, 70910-900 Brasília, Distrito Federal, Brazil.
Catholic University of Brasilia, QS 07, Lote 01, EPCT, Águas Claras, 71966-700 Brasília, Distrito Federal, Brazil.
ACS Infect Dis. 2023 Jul 14;9(7):1334-1345. doi: 10.1021/acsinfecdis.3c00076. Epub 2023 Jun 12.
Six new ether phospholipid analogues encompassing constituents from cashew nut shell liquid as the lipid portion were synthesized in an effort to valorize byproducts of the cashew industry toward the generation of potent compounds against Chagas disease. Anacardic acids, cardanols, and cardols were used as the lipid portions and choline as the polar headgroup. The compounds were evaluated for their antiparasitic activity against different developmental stages of . Compounds and were found to be the most potent against epimastigotes, trypomastigotes, and intracellular amastigotes exhibiting selectivity indices against the latter 32-fold and 7-fold higher than current drug benznidazole, respectively. Hence, four out of six analogues can be considered as hit-compounds toward the sustainable development of new treatments for Chagas disease, based on inexpensive agro-waste material.
为了利用腰果壳液的副产品，向生成对抗恰加斯病的有效化合物努力，我们合成了六种新的醚磷脂类似物，其脂质部分包含腰果壳液的成分。利用酸性没食子酸、 cardanol 和 cardol 作为脂质部分，胆碱作为极性头基。评估了这些化合物对不同发育阶段的寄生虫的抗寄生虫活性。发现化合物和对滋养体、鞭毛体和细胞内无鞭毛体最有效，对后者的选择性指数分别比目前的药物苯并咪唑高 32 倍和 7 倍。因此，基于廉价的农业废物材料，这六种类似物中有四种可以被认为是针对开发治疗恰加斯病的新疗法的有效化合物。
