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Identification of N-acyl quinolin-2(1H)-ones as new selective agents against clinical isolates of Acanthamoeba keratitis.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2020-03-23 , DOI: 10.1016/j.bioorg.2020.103791
María Reyes-Batlle 1 , Mónica Blanco Freijo 2 , Atteneri López-Arencibia 3 , Jacob Lorenzo-Morales 3 , Grant McNaughton-Smith 4 , José E Piñero 3 , Teresa Abad-Grillo 2
Affiliation  

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.

中文翻译:

N-酰基喹啉2(1H)-作为新的选择剂对抗棘阿米巴角膜炎临床分离株的鉴定。

针对一组临床相关的原生动物(利什曼原虫,锥虫和棘阿米巴)筛选了一组N-取代的喹啉2(1H)-酮。三种喹啉2(1H)-1化合物被鉴定为选择性抗棘阿米巴剂。进一步的评估表明,这些化合物对滋养体和castellanii Neff的囊肿形式均具有活性,并通过凋亡导致原生动物死亡。本文提供的数据确定N-酰基喹啉2(1H)-是一种有希望的新型选择性抗棘阿米巴剂。
更新日期:2020-04-20
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