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

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Title: Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362.
Authors: Lowe MA; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Cardenas A; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Valentin JP; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Zhu Z; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Abendroth J; UCB, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., Castro JL; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Class R; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Delaunois A; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Fleurance R; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Gerets H; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Gryshkova V; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., King L; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Lorimer DD; UCB, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., MacCoss M; Bohicket Pharma Consulting LLC, 2556 Seabrook Island Road, Seabrook Island, South Carolina 29455, United States., Rowley JH; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Rosseels ML; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Royer L; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium., Taylor RD; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Wong M; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Zaccheo O; UCB, 216 Bath Road, Slough SL1 3WE, United Kingdom., Chavan VP; Sai Life Sciences Limited, Plot DS-7, IKP Knowledge Park, Genome Valley, Turkapally, Hyderabad 500078, Telangana, India., Ghule GA; Sai Life Sciences Limited, Plot DS-7, IKP Knowledge Park, Genome Valley, Turkapally, Hyderabad 500078, Telangana, India., Tapkir BK; Sai Life Sciences Limited, Plot DS-7, IKP Knowledge Park, Genome Valley, Turkapally, Hyderabad 500078, Telangana, India., Burrows JN; Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, 1215 Geneva, Switzerland., Duffey M; Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, 1215 Geneva, Switzerland., Rottmann M; Swiss Tropical and Public Health Institute, Kreuzstrasse 2, CH-4123 Allschwil, Switzerland.; University of Basel, 4002 Basel, Switzerland., Wittlin S; Swiss Tropical and Public Health Institute, Kreuzstrasse 2, CH-4123 Allschwil, Switzerland.; University of Basel, 4002 Basel, Switzerland., Angulo-Barturen I; The Art of Discovery, SL Biscay Science and Technology Park, Astondo Bidea, BIC Bizkaia Building, no. 612, Derio 48160, Bizkaia, Basque Country, Spain., Jiménez-Díaz MB; The Art of Discovery, SL Biscay Science and Technology Park, Astondo Bidea, BIC Bizkaia Building, no. 612, Derio 48160, Bizkaia, Basque Country, Spain., Striepen J; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States., Fairhurst KJ; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States., Yeo T; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States., Fidock DA; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.; 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., Cowman AF; The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia., Favuzza P; The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia., Crespo-Fernandez B; Global Health, GlaxoSmithKline R&D, Tres Cantos, 28760 Madrid, Spain., Gamo FJ; Global Health, GlaxoSmithKline R&D, Tres Cantos, 28760 Madrid, Spain., Goldberg DE; 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., Soldati-Favre D; Department of Microbiology and Molecular Medicine, Faculty of Medicine, CMU, 1 rue Michel-Servet, CH-1211 Genève 4, Switzerland., Laleu B; Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, 1215 Geneva, Switzerland., de Haro T; UCB, Chem. du Foriest 1, 1420 Braine-l'Alleud, Belgium.
Source: Journal of medicinal chemistry [J Med Chem] 2022 Oct 27; Vol. 65 (20), pp. 14121-14143. Date of Electronic Publication: 2022 Oct 10.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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