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Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda, Sreekanth; Deng, Xiaoyi; White, Karen L; El Mazouni, Farah; White, John; Shackleford, David M; Katneni, Kasiram; Chiu, Francis C K; Barker, Helena; McLaren, Jenna; Crighton, Elly; Chen, Gong; Angulo-Barturen, Inigo; Jimenez-Diaz, Maria Belen; Ferrer, Santiago; Huertas-Valentin, Leticia; Martinez-Martinez, Maria Santos; Lafuente-Monasterio, Maria Jose; Chittimalla, Rajesh; Shahi, Shatrughan P; Wittlin, Sergio; Waterson, David; Burrows, Jeremy N; Matthews, Dave; Tomchick, Diana; Rathod, Pradipsinh K; Palmer, Michael J; Charman, Susan A; Phillips, Margaret A.
Affiliation
  • Kokkonda S; Departments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
  • Deng X; Departments of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
  • White KL; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • El Mazouni F; Departments of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
  • White J; Departments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
  • Shackleford DM; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Katneni K; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Chiu FCK; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Barker H; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • McLaren J; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Crighton E; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Chen G; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
  • Angulo-Barturen I; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Jimenez-Diaz MB; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Ferrer S; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Huertas-Valentin L; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Martinez-Martinez MS; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Lafuente-Monasterio MJ; GSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
  • Chittimalla R; Syngene International Ltd, Bangalore 560 099, India.
  • Shahi SP; Syngene International Ltd, Bangalore 560 099, India.
  • Wittlin S; Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
  • Waterson D; University of Basel, 4002 Basel, Switzerland.
  • Burrows JN; Medicines for Malaria Venture, 1215 Geneva, Switzerland.
  • Matthews D; Medicines for Malaria Venture, 1215 Geneva, Switzerland.
  • Tomchick D; Medicines for Malaria Venture, 1215 Geneva, Switzerland.
  • Rathod PK; Department of Biophysics, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
  • Palmer MJ; Departments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
  • Charman SA; Medicines for Malaria Venture, 1215 Geneva, Switzerland.
  • Phillips MA; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
J Med Chem ; 63(9): 4929-4956, 2020 05 14.
Article in En | MEDLINE | ID: mdl-32248693
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrroles / Malaria, Falciparum / Oxidoreductases Acting on CH-CH Group Donors / Enzyme Inhibitors / Antimalarials Type of study: Prognostic_studies Limits: Animals / Female / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2020 Type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrroles / Malaria, Falciparum / Oxidoreductases Acting on CH-CH Group Donors / Enzyme Inhibitors / Antimalarials Type of study: Prognostic_studies Limits: Animals / Female / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2020 Type: Article Affiliation country: United States