Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Author:

Lowe Martin A.1,Cardenas Alvaro2,Valentin Jean-Pierre2,Zhu Zhaoning1,Abendroth Jan3,Castro Jose L.1,Class Reiner2,Delaunois Annie2ORCID,Fleurance Renaud2,Gerets Helga2ORCID,Gryshkova Vitalina2,King Lloyd1,Lorimer Donald D.3,MacCoss Malcolm4,Rowley Julian H.1ORCID,Rosseels Marie-Luce2,Royer Leandro2,Taylor Richard D.1ORCID,Wong Melanie1,Zaccheo Oliver1,Chavan Vishal P.5,Ghule Gokul A.5,Tapkir Bapusaheb K.5,Burrows Jeremy N.6ORCID,Duffey Maëlle6,Rottmann Matthias78,Wittlin Sergio78,Angulo-Barturen Iñigo9,Jiménez-Díaz María Belén9,Striepen Josefine10,Fairhurst Kate J.10,Yeo Tomas10,Fidock David A.1011,Cowman Alan F.12,Favuzza Paola12,Crespo-Fernandez Benigno13,Gamo Francisco Javier13ORCID,Goldberg Daniel E.14ORCID,Soldati-Favre Dominique15,Laleu Benoît6ORCID,de Haro Teresa2ORCID

Affiliation:

1. UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom

2. UCB, Chem. du Foriest 1, 1420 Braine-l’Alleud, Belgium

3. UCB, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States

4. Bohicket Pharma Consulting LLC, 2556 Seabrook Island Road, Seabrook Island, South Carolina 29455, United States

5. Sai Life Sciences Limited, Plot DS-7, IKP Knowledge Park, Genome Valley, Turkapally, Hyderabad 500078, Telangana, India

6. Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, 1215 Geneva, Switzerland

7. Swiss Tropical and Public Health Institute, Kreuzstrasse 2, CH-4123 Allschwil, Switzerland

8. University of Basel, 4002 Basel, Switzerland

9. The Art of Discovery, SL Biscay Science and Technology Park, Astondo Bidea, BIC Bizkaia Building, no. 612, Derio 48160, Bizkaia, Basque Country, Spain

10. Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States

11. Center for Malaria Therapeutics and Antimicrobial Resistance, Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, New York 10032, United States

12. The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia

13. Global Health, GlaxoSmithKline R&D, Tres Cantos, 28760 Madrid, Spain

14. Division of Infectious Diseases, Department of Medicine, Washington University School of Medicine, 660 South Euclid Avenue, Campus Box 8051, St. Louis, Missouri 63110, United States

15. Department of Microbiology and Molecular Medicine, Faculty of Medicine, CMU, 1 rue Michel-Servet, CH-1211 Genève 4, Switzerland

Funder

UCB

Medicines for Malaria Venture

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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