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新型异弗洛醇色满酮和喹啉酮类似物作为抗利什曼原虫剂的合成与评价

Synthesis and evaluation of novel chromanone and quinolinone analogues of uniflorol as anti-leishmanial agents.

作者信息

Castro Helena, Cruz Tânia, de Aguiar Amaral Patrícia, da Silva Cardoso Paula, Alsaffar Ahmed, Farrell Patrick, Tomás Ana M, Barlow James W

机构信息

i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal.

IBMC - Instituto de Biologia Molecular e Celular, Universidade do Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal.

出版信息

Heliyon. 2020 Mar 20;6(3):e03614. doi: 10.1016/j.heliyon.2020.e03614. eCollection 2020 Mar.

DOI:10.1016/j.heliyon.2020.e03614
PMID:32258470
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7096758/
Abstract

Within this work, we describe the design and synthesis of a range of novel chromanones and quinolinones, based on natural products reported to possess anti-leishmanial action. The core heterocycles were obtained either via classical or ionic liquid mediated Kabbe condensation in the case of chromanones, or aqueous Sonogashira based alkynylation followed by acid-catalysed cyclisation in the case of quinolinones. Upon testing in promastigotes, axenic amastigotes and -infected macrophages, compound was identified as displaying interesting activity, inhibiting axenic amastigotes and intracellular amastigotes with ICs of 25.3 and 24.6μM respectively.

摘要

在这项工作中，我们描述了一系列基于据报道具有抗利什曼原虫作用的天然产物的新型色满酮和喹啉酮的设计与合成。对于色满酮，核心杂环是通过经典的或离子液体介导的卡贝缩合反应得到的；对于喹啉酮，则是通过基于水相的Sonogashira炔基化反应，随后进行酸催化环化反应得到的。在对前鞭毛体、无菌无鞭毛体和感染的巨噬细胞进行测试时，化合物被鉴定为具有有趣的活性，分别以25.3和24.6μM的半数抑制浓度抑制无菌无鞭毛体和细胞内无鞭毛体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/bd6d0a75fd6c/sc4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/1afae2c86d9a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/131b7c4d3e8c/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/9d8f215b24cf/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/78fcb6b8bca1/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/57b54affd322/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/2d139abd94b4/sc3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/bd6d0a75fd6c/sc4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/1afae2c86d9a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/131b7c4d3e8c/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/9d8f215b24cf/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/78fcb6b8bca1/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/57b54affd322/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/2d139abd94b4/sc3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/50d8/7096758/bd6d0a75fd6c/sc4.jpg

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