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Selected Works of Roland A. Cooper
Article
Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
Natural Sciences and Mathematics | Faculty Scholarship
  • Papireddy Kancharla, Department of Chemistry, Portland State University
  • Rozalia A. Dodean, Department of Veterans Affairs Medical Center
  • Yuexin Li, Department of Veterans Affairs Medical Center
  • Sovitj Pou, Department of Veterans Affairs Medical Center
  • Brandon Pybus, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Victor Melendez, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Lisa Read, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Charles E Bane, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Brian Vesely, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Mara Kreishman-Deitrick, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Chad Black, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Qigui Li, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Richard J. Sciotti, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Raul Olmeda, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Thu-Lan Luong, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Heather Gaona, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Brittney Potter, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Jason Sousa, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Sean Marcsisin, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Diana Caridha, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Lisa Xie, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Chau Vuong, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Qiang Zeng, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Jing Zhang, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Ping Zhang, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Hsiuling Lin, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Kirk Butler, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Norma Roncal, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Lacy Gaynor-Ohnstad, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Susan E. Leed, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Christina Nolan, Division of Experimental Therapeutics, Walter Reed Army Institute of Research
  • Frida G. Ceja, Department of Natural Sciences and Mathematics, Dominican University of California
  • Stephanie A. Rasmussen, Department of Natural Sciences and Mathematics, Dominican University of California
  • Patrick K. Tumwebaze, Infectious Diseases Research Collaboration
  • Philip J. Rosenthal, Department of Medicine, University of California, San Francisco
  • Jianbing Mu, Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health
  • Brett R. Bayles, Global Health Program, Dominican University of California
  • Roland A. Cooper, Department of Natural Sciences and Mathematics, Dominican University of California
  • Kevin A. Reynolds, Department of Chemistry, Portland State University
  • Martin J. Smilkstein, Department of Veterans Affairs Medical Center
  • Michael K. Riscoe, Department of Chemistry, Portland State University
  • Jane X. Kelly, Department of Chemistry, Portland State University
Link Find in your library
Department
Natural Sciences and Mathematics
Document Type
Article
Source
Journal of Medicinal Chemistry
Publication Date
6-11-2020
Disciplines
Abstract

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clinically available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria. Previously, we described a novel antimalarial acridone chemotype that is potent against both blood-stage and liver-stage malaria parasites. Here, we describe an optimization process that has produced a second-generation acridone series with significant improvements in efficacy, metabolic stability, pharmacokinetics, and safety profiles. These findings highlight the therapeutic potential of dual-stage targeting acridones as novel drug candidates for further preclinical development.

PubMed ID
32390431
Rights
Copyright © 2020 American Chemical Society
Citation Information
Papireddy Kancharla, Rozalia A. Dodean, Yuexin Li, Sovitj Pou, et al.. "Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials." Vol. 63 Iss. 11 (2020) p. 6179 - 6202 ISSN: 1520-4804
Available at: http://works.bepress.com/roland_cooper/53/