Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

Author:

Russell Stephanie1,Rahmani Raphaël2,Jones Amy J.3,Newson Harriet L.1,Neilde Kevin24,Cotillo Ignacio4,Rahmani Khajouei Marzieh1,Ferrins Lori2,Qureishi Sana1,Nguyen Nghi2,Martinez-Martinez Maria S.4,Weaver Donald F.5,Kaiser Marcel67,Riley Jennifer8,Thomas John8,De Rycker Manu8,Read Kevin D.8,Flematti Gavin R.1,Ryan Eileen9,Tanghe Scott10,Rodriguez Ana10,Charman Susan A.29,Kessler Albane4,Avery Vicky M.3,Baell Jonathan B.2,Piggott Matthew J.1

Affiliation:

1. School of Chemistry and Biochemistry, The University of Western Australia, 35 Stirling Highway, Crawley, Perth 6009, Western Australia, Australia

2. Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia

3. Eskitis Institute for Drug Discovery, Griffith University, Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia

4. GlaxoSmithKline, 28760 Tres Cantos, Spain

5. Department of Chemistry, Dalhousie University, Halifax Nova Scotia B3H 4R2, Canada

6. Swiss Tropical and Public Health Institute, Socinstrasse, 4051 Basel, Switzerland

7. University of Basel, Petesplatz 1, 4003 Basel, Switzerland

8. Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, DD1 5EH Dundee, U.K.

9. Centre for Drug Candidate Optimisation, Monash University, Parkville, Victoria 3052, Australia

10. Anti-Infectives Screening Core, New York University School of Medicine, New York, New York 10010, United States

Funder

University of Western Australia

National Health and Medical Research Council

Wellcome Trust

Tres Cantos Open Lab Foundation

Victorian State Government

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference94 articles.

1. Trypanosomiasis, Human African (Sleeping Sickness), Fact Sheet;World Health Organization:Geneva, 2016; http://www.who.int/mediacentre/factsheets/fs259/en/(accessed March 21, 2016).

2. Chagas Disease (American Trypanosomiasis), Fact Sheet;World Health Organization:Geneva, 2016; http://www.who.int/mediacentre/factsheets/fs340/en/(accessed March 21, 2106).

3. Putting sleeping sickness to bed

4. East African Trypanosomiasis FAQs;Centers for Disease Control and Prevention:Atlanta, GA, 2012; http://www.cdc.gov/parasites/sleepingsickness/gen_info/faqs-east.html(accessed March 20, 2016) .

5. West African Trypanosomiasis FAQs;Centers for Disease Control:Atlanta, GA, 2012; http://www.cdc.gov/parasites/sleepingsickness/gen_info/faqs-west.html(accessed March 20, 2016) .

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