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Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach, Claire; Dam, Jean; Woodland, John G; Kaur, Gurminder; Khonde, Lutete P; Brunschwig, Christel; Njoroge, Mathew; Wicht, Kathryn J; Horatscheck, André; Paquet, Tanya; Boyle, Grant A; Gibhard, Liezl; Taylor, Dale; Lawrence, Nina; Yeo, Tomas; Mok, Sachel; Eastman, Richard T; Dorjsuren, Dorjbal; Talley, Daniel C; Guo, Hui; Simeonov, Anton; Reader, Janette; van der Watt, Mariëtte; Erlank, Erica; Venter, Nelius; Zawada, Jacek W; Aswat, Ayesha; Nardini, Luisa; Coetzer, Theresa L; Lauterbach, Sonja B; Bezuidenhout, Belinda C; Theron, Anjo; Mancama, Dalu; Koekemoer, Lizette L; Birkholtz, Lyn-Marie; Wittlin, Sergio; Delves, Michael; Ottilie, Sabine; Winzeler, Elizabeth A; von Geldern, Thomas W; Smith, Dennis; Fidock, David A; Street, Leslie J; Basarab, Gregory S; Duffy, James; Chibale, Kelly.
Afiliação
  • Le Manach C; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Dam J; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Woodland JG; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Kaur G; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Khonde LP; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Brunschwig C; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • Njoroge M; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • Wicht KJ; Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
  • Horatscheck A; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Paquet T; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Boyle GA; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
  • Gibhard L; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • Taylor D; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • Lawrence N; Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
  • Yeo T; Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
  • Mok S; Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
  • Eastman RT; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
  • Dorjsuren D; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
  • Talley DC; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
  • Guo H; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
  • Simeonov A; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
  • Reader J; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • van der Watt M; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • Erlank E; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Venter N; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Zawada JW; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Aswat A; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Nardini L; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Coetzer TL; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Lauterbach SB; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Bezuidenhout BC; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Theron A; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Mancama D; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Koekemoer LL; Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Birkholtz LM; Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Wittlin S; Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Delves M; Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa.
  • Ottilie S; Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa.
  • Winzeler EA; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • von Geldern TW; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.
  • Smith D; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • Fidock DA; Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
  • Street LJ; University of Basel, 4003 Basel, Switzerland.
  • Basarab GS; Imperial College London, South Kensington, London SW7 2AZ, U.K.
  • Duffy J; London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K.
  • Chibale K; Division of Host-Microbe Systems & Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093-076, United States.
J Med Chem ; 64(4): 2291-2309, 2021 02 25.
Article em En | MEDLINE | ID: mdl-33573376
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Compostos de Espiro / Antimaláricos Tipo de estudo: Diagnostic_studies Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: África do Sul
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Compostos de Espiro / Antimaláricos Tipo de estudo: Diagnostic_studies Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: África do Sul