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.

Autor: 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.; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa., Venter N; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.; 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.; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa., Aswat A; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.; 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.; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa., Coetzer TL; 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., Lauterbach SB; 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., Bezuidenhout BC; 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., Theron A; Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa., Mancama D; Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa., Koekemoer LL; Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.; Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa., Birkholtz LM; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa., Wittlin S; Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.; University of Basel, 4003 Basel, Switzerland., Delves M; Imperial College London, South Kensington, London SW7 2AZ, U.K.; London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K., Ottilie S; Division of Host-Microbe Systems & Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093-076, United States., Winzeler EA; Division of Host-Microbe Systems & Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093-076, United States., von Geldern TW; Embedded Consulting, P.O. Box 726, Richmond, Illinois 60071, United States., Smith D; 4 The Maltings, Walmer CT14 7AR, U.K., Fidock DA; Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.; Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, New York 10032, United States., Street LJ; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa., Basarab GS; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa., Duffy J; Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland., Chibale K; Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.; South African Medical Research Council, Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Feb 25; Vol. 64 (4), pp. 2291-2309. Date of Electronic Publication: 2021 Feb 12.

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials.

Autor: van der Watt ME; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Reader J; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Churchyard A; Plasmodium Molecular Research Unit, Wits Research Institute for Malaria, Department of Molecular Medicine and Haematology, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand and National Health Laboratory Service, Johannesburg 2193, South Africa., Nondaba SH; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Lauterbach SB; Plasmodium Molecular Research Unit, Wits Research Institute for Malaria, Department of Molecular Medicine and Haematology, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand and National Health Laboratory Service, Johannesburg 2193, South Africa., Niemand J; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Abayomi S; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., van Biljon RA; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Connacher JI; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., van Wyk RDJ; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa., Le Manach C; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa., Paquet T; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa., González Cabrera D; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa., Brunschwig C; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa., Theron A; Biosciences, Council for Scientific and Industrial Research, PO Box 395, Pretoria 0001, South Africa., Lozano-Arias S; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain., Rodrigues JFI; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain., Herreros E; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain., Leroy D; Medicines for Malaria Venture, International Center Cointrin, Route de Pré-Bois 20, 1215, Geneva, Switzerland., Duffy J; Medicines for Malaria Venture, International Center Cointrin, Route de Pré-Bois 20, 1215, Geneva, Switzerland., Street LJ; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa., Chibale K; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.; South African Medical Research Council, Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa., Mancama D; Biosciences, Council for Scientific and Industrial Research, PO Box 395, Pretoria 0001, South Africa., Coetzer TL; Plasmodium Molecular Research Unit, Wits Research Institute for Malaria, Department of Molecular Medicine and Haematology, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand and National Health Laboratory Service, Johannesburg 2193, South Africa., Birkholtz LM; Department of Biochemistry, Institute for Sustainable Malaria Control and South African Medical Research Council Collaborating Centre for Malaria Research, University of Pretoria, Private Bag x20, Hatfield, Pretoria 0028, South Africa.

Publikováno v: The Journal of antimicrobial chemotherapy [J Antimicrob Chemother] 2018 May 01; Vol. 73 (5), pp. 1279-1290.

Receptor-based identification of an inhibitory peptide against blood stage malaria.

Autor: Li X; Department of Pharmacology and Cancer Center, University of Illinois College of Medicine, 909 South Wolcott Avenue, Room 5100, MC 704, Chicago, IL 60612, USA., Chen H, Khan AA, Lauterbach SB, Lanzillotti R, Rai PR, Kane RS, Coetzer TL, Chishti AH

Publikováno v: Biochemical and biophysical research communications [Biochem Biophys Res Commun] 2008 Nov 21; Vol. 376 (3), pp. 489-93. Date of Electronic Publication: 2008 Sep 13.