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Updated: Jul 25, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
2-Aroyl quinazolinone: Synthesis and in vitro anti-parasitic activity
Koketso J Setshedi1, Richard M Beteck1, Omobolanle J Jesumoroti1
1Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
Abstract:
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 IC50 values of 4.7 μM (T. b. brucei) and 1.1 μM (T. b. rhodesiense), respectively.

