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2-Aroyl quinazolinone: Synthesis and in vitro anti-parasitic activity.
Setshedi, Koketso J; Beteck, Richard M; Jesumoroti, Omobolanle J; Ilbeigi, Kayhan; Mabille, Dorien; Caljon, Guy; Van der Kooy, Frank; Legoabe, Lesetja J.
Afiliación
  • Setshedi KJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
  • Beteck RM; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
  • Jesumoroti OJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
  • Ilbeigi K; Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium.
  • Mabille D; Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium.
  • Caljon G; Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium.
  • Van der Kooy F; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
  • Legoabe LJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
Chem Biol Drug Des ; 102(4): 763-772, 2023 10.
Article en En | MEDLINE | ID: mdl-37353860
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Contexto en salud: 3_ND Problema de salud: 3_chagas_disease / 3_neglected_diseases / 3_trypanosomiasis Asunto principal: Parásitos / Trypanosoma brucei brucei / Trypanosoma cruzi / Leishmania infantum / Antiprotozoarios Límite: Animals / Humans Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: Sudáfrica

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Contexto en salud: 3_ND Problema de salud: 3_chagas_disease / 3_neglected_diseases / 3_trypanosomiasis Asunto principal: Parásitos / Trypanosoma brucei brucei / Trypanosoma cruzi / Leishmania infantum / Antiprotozoarios Límite: Animals / Humans Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: Sudáfrica
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