Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

• Le Manach C Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Nchinda AT Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Paquet T Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Gonzàlez Cabrera D Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Younis Y Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Han Z Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Bashyam S Syngene International Ltd. , Biocon Park, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560099, India.
• Zabiulla M Syngene International Ltd. , Biocon Park, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560099, India.
• Taylor D Division of Clinical Pharmacology, Department of Medicine, University of Cape Town , Observatory, Cape Town, 7925, South Africa.
• Lawrence N Division of Clinical Pharmacology, Department of Medicine, University of Cape Town , Observatory, Cape Town, 7925, South Africa.
• White KL Centre for Drug Candidate Optimisation, Monash University , 381 Royal Parade, Parkville, Victoria 3052 Australia.
• Charman SA Centre for Drug Candidate Optimisation, Monash University , 381 Royal Parade, Parkville, Victoria 3052 Australia.
• Waterson D Medicines for Malaria Venture , ICC, Route de Pré-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland.
• Witty MJ Medicines for Malaria Venture , ICC, Route de Pré-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland.
• Wittlin S Swiss Tropical and Public Health Institute , Socinstrasse 57, 4002 Basel, Switzerland.
• Botha ME Department of Biochemistry, Centre for Sustainable Malaria Control, University of Pretoria , Private Bag X20, Hatfield 0028, South Africa.
• Nondaba SH Department of Biochemistry, Centre for Sustainable Malaria Control, University of Pretoria , Private Bag X20, Hatfield 0028, South Africa.
• Reader J Department of Biochemistry, Centre for Sustainable Malaria Control, University of Pretoria , Private Bag X20, Hatfield 0028, South Africa.
• Birkholtz LM Department of Biochemistry, Centre for Sustainable Malaria Control, University of Pretoria , Private Bag X20, Hatfield 0028, South Africa.
• Jiménez-Díaz MB GlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain.
• Martínez MS GlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain.
• Ferrer S GlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain.
• Angulo-Barturen I GlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain.
• Meister S Department of Pediatrics, Pharmacology and Drug Discovery, School of Medicine, University of California, San Diego (UCSD) , 9500 Gilman Drive, La Jolla, California 92093, United States.
• Antonova-Koch Y Department of Pediatrics, Pharmacology and Drug Discovery, School of Medicine, University of California, San Diego (UCSD) , 9500 Gilman Drive, La Jolla, California 92093, United States.
• Winzeler EA Department of Pediatrics, Pharmacology and Drug Discovery, School of Medicine, University of California, San Diego (UCSD) , 9500 Gilman Drive, La Jolla, California 92093, United States.
• Street LJ Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
• Chibale K Drug Discovery and Development Center (H3D), Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.

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Animals

Antimalarials

Disease Models, Animal

Dose-Response Relationship, Drug

Ether-A-Go-Go Potassium Channels

Hep G2 Cells

Humans

Life Cycle Stages

Malaria

Mice

Mice, SCID

Microsomes, Liver

Molecular Structure

Parasitic Diseases, Animal

Parasitic Sensitivity Tests

Plasmodium berghei

Plasmodium falciparum

Pyrazines

Solubility

Structure-Activity Relationship

Water