Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model

Author:

Singh Kawaljit12,Okombo John1,Brunschwig Christel3,Ndubi Ferdinand1,Barnard Linley1,Wilkinson Chad1,Njogu Peter M.4,Njoroge Mathew3,Laing Lizahn3,Machado Marta5,Prudêncio Miguel5,Reader Janette6,Botha Mariette6,Nondaba Sindisiwe6,Birkholtz Lyn-Marie6,Lauterbach Sonja7,Churchyard Alisje7,Coetzer Theresa L.7,Burrows Jeremy N.8,Yeates Clive9,Denti Paolo3,Wiesner Lubbe3,Egan Timothy J.1ORCID,Wittlin Sergio1011,Chibale Kelly12ORCID

Affiliation:

1. Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa

2. 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

3. Department of Medicine, Division of Clinical Pharmacology, University of Cape Town, Observatory, 7925, South Africa

4. Department of Pharmaceutical Chemistry, University of Nairobi, P.O. Box 19676, Nairobi, 00202, Kenya

5. Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal

6. Department of Biochemistry, Institute for Sustainable Malaria Control, University of Pretoria, Private Bag X20, Hatfield 0028, South Africa

7. Wits Research Institute for Malaria, Faculty of Health Sciences, University of the Witwatersrand and National Health Laboratory Service, Johannesburg 2193, South Africa

8. Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland

9. Inpharma Consultancy, 6 Dudley Hill Close, Welwyn, Hertfordshire AL60QQ, U.K.

10. Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland

11. University of Basel, 4003 Basel, Switzerland

Funder

University of Cape Town

Department of Science and Technology, Republic of South Africa

South African Medical Research Council

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference27 articles.

1. World Health Organization (WHO). World Malaria Report 2015. http://www.who.int/malaria/publications/world-malaria-report-2015/report/en/(accessed September 24, 2016) .

2. The silent path to thousands of merozoites: the Plasmodium liver stage

3. Artemisinin Resistance inPlasmodium falciparumMalaria

4. Evidence of Artemisinin-Resistant Malaria in Western Cambodia

5. The Combinatorial Synthesis of Bicyclic Privileged Structures or Privileged Substructures

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