2-Aroyl quinazolinone: Synthesis and in vitro anti-parasitic activity

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.

Keywords: 2-Aroyl quinazolinone derivatives; anti-leishmanial activity; anti-trypanosomal activity; one-pot oxidation.