Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics

Author:

Klug Dana M.1,Tschiegg Laura1,Diaz Rosario2,Rojas-Barros Domingo2,Perez-Moreno Guiomar2,Ceballos Gloria2,García-Hernández Raquel2,Martinez-Martinez Maria Santos3,Manzano Pilar3,Ruiz Luis Miguel2,Caffrey Conor R.4,Gamarro Francisco2,Pacanowska Dolores Gonzalez2,Ferrins Lori1ORCID,Navarro Miguel2,Pollastri Michael P.1ORCID

Affiliation:

1. Department of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States

2. Instituto de Parasitología y Biomedicina “López-Neyra”, Consejo Superior de Investigaciones Cientificas (CSIC), Granada 18016, Spain

3. Diseases of the Developing World (DDW), Tres Cantos Medicines Development Campus, GlaxoSmithKline, Tres Cantos 28760, Spain

4. Center for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States

Funder

Ministerio de Econom?a y Competitividad

National Institute of Allergy and Infectious Diseases

American Chemical Society

Instituto de Salud Carlos III

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference10 articles.

1. World Health Organization. Neglected Tropical Diseases. http://www.who.int/neglected_diseases/diseases/en/ (accessed November 24, 2015).

2. Human African trypanosomiasis

3. aDrugs for Neglected Diseases Initiative. Fexinidazole (HAT). http://www.dndi.org/diseases-projects/portfolio/fexinidazole/ (accessed February 13, 2018).

4. Oral fexinidazole for late-stage African Trypanosoma brucei gambiense trypanosomiasis: a pivotal multicentre, randomised, non-inferiority trial

5. cDrugs for Neglected Diseases Initiative. Acoziborole. http://www.dndi.org/diseases-projects/portfolio/scyx-7158/ (accessed February 13, 2017).

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