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Export Trypanosomes and Leishmania are parasitic protozoans that affect millions of people globally. Herein we report the synthesis of 2-aroyl quinazolinones and their antiprotozoal efficacy against Trypanosoma brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania infantum. These compounds were counter-screened against a human cell line for cytotoxicity. Thirteen of the twenty target compounds in this study inhibited the growth of these parasites, with compounds KJ1, and KJ10 exhibiting IC(50) values of 4.7 muM (T. b. brucei) and 1.1 muM (T. b. rhodesiense), respectively.
SEEK ID: https://fairdomhub.org/publications/730
PubMed ID: 37353860
Projects: WG1 - Compound libraries coordination and integration of compound design, WG2 - Integration of early phase studies and low environmental impact ac..., WG3 - Coordination of in vitro-to-in vivo translation of OneHealth leads..., WG4 - Integration of R&D process-environmental studies and translation i...
Publication type: Journal Article
Journal: Chem Biol Drug Des
Citation: Chem Biol Drug Des. 2023 Oct;102(4):763-772. doi: 10.1111/cbdd.14284. Epub 2023 Jun 23.
Date Published: 13th Sep 2023
Registered Mode: by PubMed ID
SubmitterViews: 17
Created: 13th Jul 2026 at 13:03
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https://orcid.org/0000-0002-4870-3202