4.7 Article

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

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BIOORGANIC CHEMISTRY
卷 99, 期 -, 页码 -

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ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103791

关键词

Protozoa; Acanthamoeba; N-acyl quinolin-2(1H)-ones; Trophozoites; Cysts

资金

  1. Organic Chemistry Department, Universidad de La Laguna
  2. RICET (Redes Tematicas de Investigacion Cooperativa, FIS) [RD16/0027/0001]
  3. Agustin de Betancourt Program

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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.

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