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Discovery of a novel lead structure for anti-malarials
Authors:Wiesner J  Wissner P  Dahse H M  Jomaa H  Schlitzer M
Institution:1. Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, D-35032 Marburg, Germany;2. Biochemisches Institut der Universitätsklinik Gießen, Friedrichstraße 24, D-35249 Gießen, Germany;3. Hans-Knöll-Institut für Naturstoff-Forschung e. V., Beutenbergstraße 11, D-07745 Jena, Germany;1. Departments of Chemistry and Immunology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA;2. Discovery Biology, Takeda San Diego, Inc., 10410 Science Center Drive, San Diego, CA 92121, USA;1. Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and College of Pharmaceutical Sciences, Soochow University, Suzhou, Jiangsu 215021, PR China;2. Cyrus Tang Hematology Center, Jiangsu Institute of Hematology, First Affiliated Hospital, and Collaborative Innovation Center of Hematology, Soochow University, Suzhou 215123, PR China;3. BeiGene (Beijing) Co., Ltd, No. 30 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, PR China;1. College of Sericulture, Textile and Biomass Sciences, Southwest University, Chongqing 400715, China;2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;3. Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN 55414, USA;4. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China;1. Laboratory for Characterization and Processing of Polymers (LCPP), Faculty of Mechanical Engineering, University of Maribor, Maribor, Slovenia;2. Institute for Chemistry and Technology of Biobased Systems, Graz University of Technology, Stremayrgasse 9, A-8010, Graz, Austria;3. Institute of Bioproducts and Paper Technology (BPTI), Graz University of Technology, Inffeldgasse 23, AT - 8010, Graz, Austria;4. Chair of Chemistry of Polymeric Materials, University of Leoben, Otto-Glöckel-Straße 2, A-8700, Leoben, Austria;5. Center of Excellence for Polysaccharide Research, Institute of Organic Chemistry and Macromolecular Chemistry, Friedrich Schiller University of Jena, Humboldtstraße 10, D-07743, Jena, Germany
Abstract:From a library of 61 compounds available from former studies 2,5-bis-acylaminobenzophenone 7p was identified as a lead structure for a novel class of anti-malaria agents active against multi-resistant Plasmodium falciparum strain Dd2. Some structural modifications of this initial lead demonstrated the potential for further improvement of the anti-plasmodial activity of this novel class of anti-malarials.
Keywords:
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