Catechol Pyrazolinones as Trypanocidals: Fragment-Based Design, Synthesis, and Pharmacological Evaluation of Nanomolar Inhibitors of Trypanosomal Phosphodiesterase B1

Author:

Orrling Kristina M.1,Jansen Chimed1,Vu Xuan Lan2,Balmer Vreni3,Bregy Patrick2,Shanmugham Anitha4,England Paul4,Bailey David4,Cos Paul5,Maes Louis5,Adams Emily6,van den Bogaart Erika6,Chatelain Eric7,Ioset Jean-Robert7,van de Stolpe Andrea1,Zorg Stèphanie1,Veerman Johan8,Seebeck Thomas2,Sterk Geert Jan8,de Esch Iwan J. P.1,Leurs Rob1

Affiliation:

1. Leiden/Amsterdam Centre of Drug Research (LACDR), Amsterdam Institute of Molecules, Medicines and Systems (AIMMS), Division of Medicinal Chemistry, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands

2. Institute of Cell Biology, University of Bern, Baltzerstrasse 4, 3012 Bern, Switzerland

3. Institute of Parasitology of the University of Bern, University of Bern, Baltzerstrasse 4, 3012 Bern, Switzerland

4. IOTA Pharmaceuticals, St. John’s Innovation Centre, Cowley Road, Cambridge CB4 0WS, United Kingdom

5. Laboratory for Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Groenenborgerlaan 171, 2020 Wilrijk, Belgium

6. Department of Biomedical Research, Royal Tropical Institute Amsterdam, Meibergdreef 39, 1105 AZ Amsterdam, The Netherlands

7. DNDi (Drugs for Neglected Diseases initiative), 15 Chemin Louis Dunant, 1202 Geneva, Switzerland

8. Mercachem, P.O. Box 6747, 6503 GE Nijmegen, The Netherlands

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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