Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites |
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| Affiliation: | 1. Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan;2. Synstar Japan Co., Ltd, Orbic Bldg 3F, 2-9-46 Sakaecho, Odawara 250-0011, Japan;3. College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215006, China;4. Center for Advanced Research in Sciences, University of Dhaka, Bangladesh;5. Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland;6. University of Basel, CH-4003 Basel, Switzerland;7. School of Medicine, Department of Infection and Immunity, Division of Medical Zoology, Jichi Medical University, 3311-1 Yakushiji, Shimotsuke-shi 329-0498, Japan;1. University of Colorado at Boulder, Department of Psychology, United States;2. eCortex, Inc., Boulder, CO, USA;3. Carnegie Mellon University, Department of Psychology, United States;4. Denver University, United States;3. Center for Plant Lipid Research, Department of Biological Sciences, University of North Texas, Denton, Texas 76203;4. Department of Chemistry, the City College of New York. New York, New York 10031;5. Vision Research Center, Department of Ophthalmology, School of Medicine, University of Missouri, Kansas City, Missouri 64108;6. Plant Biology Division, Samuel Roberts Noble Foundation, Ardmore, Oklahoma 73401;1. Department of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada;2. Department of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA |
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| Abstract: | A productive synthesis of benzo[a]phenoxazine derivative SSJ-183 (1), a promising lead for antimalarial agents, was developed using a one pot procedure. Furthermore, N-deethylated metabolite 3 and bis-N,N-deethylated metabolite 4 were synthesized by the application of the method. The metabolites 3 and 4 showed comparable and ∼2-fold increased activities against drug-sensitive and drug-resistant Plasmodium falciparum parasites. |
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| Keywords: | Antimalarial Metabolites Drug-sensitive and drug-resistant |
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