2‐Aroyl quinazolinone: Synthesis and in vitro anti‐parasitic activity-Reference-Cited by-同舟云学术

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

Published:2023-06-23 Issue:4 Volume:102 Page:763-772
ISSN:1747-0277
Container-title:Chemical Biology & Drug Design
language:en
Short-container-title:Chem Biol Drug Des

Author:

Setshedi Koketso J.¹,Beteck Richard M.¹,Jesumoroti Omobolanle J.¹,Ilbeigi Kayhan²,Mabille Dorien²,Caljon Guy²,Van der Kooy Frank¹,Legoabe Lesetja J.¹^ORCID

Affiliation:

1. Centre of Excellence for Pharmaceutical Sciences North‐West University Potchefstroom South Africa

2. Laboratory of Microbiology, Parasitology and Hygiene, Infla‐Med Centre of Excellence University of Antwerp Antwerp Belgium

Abstract

AbstractTrypanosomes 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.

Funder

National Research Foundation

Publisher

Wiley

Subject

Molecular Medicine,Biochemistry,Drug Discovery,Pharmacology,Organic Chemistry

Link

https://onlinelibrary.wiley.com/doi/pdf/10.1111/cbdd.14284

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