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Discovery of antiplasmodial pyridine carboxamides and thiocarboxamides.
Redway, Alexa; Spry, Christina; Brown, Ainka; Wiedemann, Ursula; Fathoni, Imam; Garnie, Larnelle F; Qiu, Deyun; Egan, Timothy J; Lehane, Adele M; Jackson, Yvette; Saliba, Kevin J; Downer-Riley, Nadale.
Afiliação
  • Redway A; Department of Chemistry, The University of the West Indies, Mona, Kingston 7, Jamaica; Chemistry Divison, University of Technology, 237 Old Hope Road, Kingston 6, Jamaica.
  • Spry C; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Brown A; Department of Chemistry, The University of the West Indies, Mona, Kingston 7, Jamaica.
  • Wiedemann U; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Fathoni I; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Garnie LF; Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa.
  • Qiu D; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Egan TJ; Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, Faculty of Health Sciences, University of Cape Town, Observatory, 7925, South Africa.
  • Lehane AM; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Jackson Y; Department of Chemistry, The University of the West Indies, Mona, Kingston 7, Jamaica.
  • Saliba KJ; Research School of Biology, The Australian National University, Canberra, ACT, 2601, Australia.
  • Downer-Riley N; Department of Chemistry, The University of the West Indies, Mona, Kingston 7, Jamaica. Electronic address: nadale.downer02@uwimona.edu.jm.
Int J Parasitol Drugs Drug Resist ; 25: 100536, 2024 Aug.
Article em En | MEDLINE | ID: mdl-38663046
ABSTRACT
Malaria continues to be a significant burden, particularly in Africa, which accounts for 95% of malaria deaths worldwide. Despite advances in malaria treatments, malaria eradication is hampered by insecticide and antimalarial drug resistance. Consequently, the need to discover new antimalarial lead compounds remains urgent. To help address this need, we evaluated the antiplasmodial activity of twenty-two amides and thioamides with pyridine cores and their non-pyridine analogues. Twelve of these compounds showed in vitro anti-proliferative activity against the intraerythrocytic stage of Plasmodium falciparum, the most virulent species of Plasmodium infecting humans. Thiopicolinamide 13i was found to possess submicromolar activity (IC50 = 142 nM) and was >88-fold less active against a human cell line. The compound was equally effective against chloroquine-sensitive and -resistant parasites and did not inhibit ß-hematin formation, pH regulation or PfATP4. Compound 13i may therefore possess a novel mechanism of action.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Piridinas / Antimaláricos Limite: Humans Idioma: En Revista: Int J Parasitol Drugs Drug Resist Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Jamaica País de publicação: Holanda
Texto completo
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XML
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Piridinas / Antimaláricos Limite: Humans Idioma: En Revista: Int J Parasitol Drugs Drug Resist Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Jamaica País de publicação: Holanda