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鉴定 N-酰基喹啉-2(1H)-酮类化合物作为抗棘阿米巴角膜炎临床分离株的新型选择性试剂。

Identification of N-acyl quinolin-2(1H)-ones as new selective agents against clinical isolates of Acanthamoeba keratitis.

机构信息

Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Laboratorio de Quimioterapias de Protozoos, Universidad de La Laguna, Tenerife, Spain.

Instituto Universitario de Bio-Orgánica 'Antonio González', Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez 2, 38206 La Laguna, Tenerife, Spain.

出版信息

Bioorg Chem. 2020 Jun;99:103791. doi: 10.1016/j.bioorg.2020.103791. Epub 2020 Mar 23.

Abstract

A collection of N-substituted quinolin-2(1H)-ones were screened against a panel of clinically relevant protozoa (Leishmania, Trypanosoma and Acanthamoeba). Three quinolin-2(1H)-one compounds were identified as selective anti-Acanthamoeba agents. Further assessment revealed that these compounds were active against both trophozoite and cyst forms of A. castellanii Neff, and caused protozoa death via apoptosis. The data presented herein identify N-acyl quinolin-2(1H)-ones as a promising new class of selective anti-Acanthamoeba agents.

摘要

我们筛选了一组 N-取代的喹啉-2(1H)-酮类化合物,以评估它们对一组临床相关的原生动物(利什曼原虫、锥虫和棘阿米巴)的活性。三种喹啉-2(1H)-酮类化合物被鉴定为选择性抗棘阿米巴的药物。进一步的评估表明,这些化合物对滋养体和包囊形式的棘阿米巴原虫 Neff 均具有活性,并通过细胞凋亡导致原生动物死亡。本文所呈现的数据表明,N-酰基喹啉-2(1H)-酮类化合物是一种有前途的新型选择性抗棘阿米巴药物。

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