New Transmission-Selective Antimalarial Agents through Hit-to-Lead Optimization of 2-([1,1'-Biphenyl]-4-carboxamido)benzoic Acid Derivatives.

Autor: Reader J; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa., Opperman DFL; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa., van der Watt ME; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa.; School of Health Systems and Public Health, University of Pretoria, Hatfield, Pretoria, 0028, South Africa., Theron A; Next Generation Health, Council for Scientific and Industrial Research, Pretoria, 0001, South Africa., Leshabane M; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa., da Rocha S; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa., Turner J; Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA., Garrabrant K; Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA., Piña I; Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA., Mills C; Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA., Woster PM; Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA., Birkholtz LM; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Lynnwood Road, Pretoria, 0028, South Africa.

Publikováno v: Chembiochem : a European journal of chemical biology [Chembiochem] 2022 Nov 04; Vol. 23 (21), pp. e202200427. Date of Electronic Publication: 2022 Oct 06.

Streamlined and Robust Stage-Specific Profiling of Gametocytocidal Compounds Against Plasmodium falciparum .

Autor: Reader J; Department of Biochemistry, Genetics and Microbiology, University of Pretoria, Pretoria, South Africa., van der Watt ME; Department of Biochemistry, Genetics and Microbiology, University of Pretoria, Pretoria, South Africa.; Institute for Sustainable Malaria Control, School of Health Systems and Public Health, University of Pretoria, Pretoria, South Africa., Birkholtz LM; Department of Biochemistry, Genetics and Microbiology, University of Pretoria, Pretoria, South Africa.

Publikováno v: Frontiers in cellular and infection microbiology [Front Cell Infect Microbiol] 2022 Jun 30; Vol. 12, pp. 926460. Date of Electronic Publication: 2022 Jun 30 (Print Publication: 2022).

The Artemiside-Artemisox-Artemisone-M1 Tetrad: Efficacies against Blood Stage P. falciparum Parasites, DMPK Properties, and the Case for Artemiside.

Autor: Gibhard L; H3D, Department of Chemistry, University of Cape Town, Observatory, Cape Town 7925, South Africa., Coertzen D; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Pretoria 0028, South Africa., Reader J; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Pretoria 0028, South Africa., van der Watt ME; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Pretoria 0028, South Africa., Birkholtz LM; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Pretoria 0028, South Africa., Wong HN; Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences, North-West University, Potchefstroom 2520, South Africa., Batty KT; Curtin Medical School, Curtin University, Bentley 6102, Australia., Haynes RK; Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences, North-West University, Potchefstroom 2520, South Africa., Wiesner L; Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, Cape Town 7925, South Africa.

Publikováno v: Pharmaceutics [Pharmaceutics] 2021 Dec 03; Vol. 13 (12). Date of Electronic Publication: 2021 Dec 03.

Naphthylisoquinoline alkaloids, validated as hit multistage antiplasmodial natural products.

Autor: Moyo P; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa., Shamburger W; Institute of Organic Chemistry, University of Würzburg, Am Hubland, 97074, Würzburg, Germany., van der Watt ME; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa., Reader J; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa., de Sousa ACC; Department of Chemistry, Faculty of Science, University of Cape Town, Rondebosch, 7701, South Africa., Egan TJ; Department of Chemistry, Faculty of Science, University of Cape Town, Rondebosch, 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory, 7925, South Africa., Maharaj VJ; Department of Chemistry, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa., Bringmann G; Institute of Organic Chemistry, University of Würzburg, Am Hubland, 97074, Würzburg, Germany; Department of Chemistry, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa. Electronic address: bringman@chemie.uni-wuerzburg.de., Birkholtz LM; Malaria Parasite Molecular Laboratory, Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, Faculty of Natural and Agricultural Sciences, University of Pretoria, Private Bag x20, Hatfield, 0028, South Africa. Electronic address: lbirkholtz@up.ac.za.

Publikováno v: International journal for parasitology. Drugs and drug resistance [Int J Parasitol Drugs Drug Resist] 2020 Aug; Vol. 13, pp. 51-58. Date of Electronic Publication: 2020 May 24.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Autor: Brunschwig C; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Lawrence N; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Taylor D; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Abay E; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Njoroge M; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Basarab GS; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Le Manach C; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa., Paquet T; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa., Gonzàlez Cabrera D; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa., Nchinda AT; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa., de Kock C; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Wiesner L; Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Denti P; Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa., Waterson D; Medicines for Malaria Venture, Geneva, Switzerland., Blasco B; Medicines for Malaria Venture, Geneva, Switzerland., Leroy D; Medicines for Malaria Venture, Geneva, Switzerland., Witty MJ; Medicines for Malaria Venture, Geneva, Switzerland., Donini C; Medicines for Malaria Venture, Geneva, Switzerland., Duffy J; Medicines for Malaria Venture, Geneva, Switzerland., Wittlin S; Swiss Tropical and Public Health Institute, Basel, Switzerland.; University of Basel, Basel, Switzerland., White KL; Centre for Drug Candidate Optimisation, Monash University, Melbourne, Victoria, Australia., Charman SA; Centre for Drug Candidate Optimisation, Monash University, Melbourne, Victoria, Australia., Jiménez-Díaz MB; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Madrid, Spain., Angulo-Barturen I; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Madrid, Spain., Herreros E; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Madrid, Spain., Gamo FJ; GlaxoSmithKline, Tres Cantos Medicines Development Campus, Madrid, Spain., Rochford R; Department of Immunology and Microbiology, University of Colorado, Aurora, Colorado, USA., Mancama D; Biosciences, Council for Scientific and Industrial Research, Pretoria, 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, South Africa., 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, Pretoria, 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, Pretoria, 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, Pretoria, South Africa., Marsh KC; AbbVie, North Chicago, Illinois, USA., Solapure SM; Nagarjuna Gardens, Bangalore, India., Burke JE; Department of Biochemistry and Microbiology, University of Victoria, Victoria, BC, Canada., McPhail JA; Department of Biochemistry and Microbiology, University of Victoria, Victoria, BC, Canada., Vanaerschot M; Department of Microbiology and Immunology, Columbia University Medical Center, New York, New York, USA., Fidock DA; Department of Microbiology and Immunology, Columbia University Medical Center, New York, New York, USA.; Division of Infectious Diseases, Department of Medicine, Columbia University Medical Center, New York, New York, USA., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, Faculty of Brain Sciences, University College London, London, United Kingdom., Siegl P; Siegl Pharma Consulting LLC, Blue Bell, Pennsylvania, USA., Smith DA; Independent Researcher, Walmer, Kent, United Kingdom., Wirjanata G; Global and Tropical Health Division, Menzies School of Health Research, Charles Darwin University, Darwin, Australia., Noviyanti R; Eijkman Institute for Molecular Biology, Jakarta, Indonesia., Price RN; Global and Tropical Health Division, Menzies School of Health Research, Charles Darwin University, Darwin, Australia.; Centre for Tropical Medicine and Global Health, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom., Marfurt J; Global and Tropical Health Division, Menzies School of Health Research, Charles Darwin University, Darwin, Australia., Silue KD; Centre Suisse de Recherches Scientifiques en Côte d'Ivoire, Abidjan, Côte d'Ivoire., Street LJ; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa., Chibale K; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch, South Africa kelly.chibale@uct.ac.za.; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch, South Africa.; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry, University of Cape Town, Rondebosch, South Africa.

Publikováno v: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2018 Oct 24; Vol. 62 (11). Date of Electronic Publication: 2018 Oct 24 (Print Publication: 2018).