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Volume 82, Issue 1
Received, 11th June, 2010, Accepted, 8th July, 2010, Published online, 9th July, 2010. |
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| Boromycin Derivatives: Synthesis and Antimalarial Activity in vitro and in vivo |
Ayumi Tsutsui, Yujiro Furuya, Tomoyasu Hirose, Riyon Kim, Rokurou Masuma, Atsuko Matsumoto, Yoko Takahashi, Aki Ishiyama, Miyuki Namatame, Kazuhiko Otoguro, Satoshi Ōmura,* and Toshiaki Sunazuka*
Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan |
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Abstract
Derivatives of boromycin, which has significant antimalarial properties both in vitro and in vivo, were examined for similar the efficacy against both drug-resistance strain and drug-sensitive strain of malaria and as a means to elucidate structure-activity relationships. More potent in vitro compounds tended to lose their properties in vivo when administered orally. Some novel 16-O-acyl derivatives were found to be more potent and selective antimalarial compounds compared to boromycin. Furthermore, alkyne-bearing 16-O-alkylacyl compounds retained reasonably good efficacy in vivo when given per os. |
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Graphical Abstract
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| Corresponding author; email: sunazuka@lisci.kitasato-u.ac.jp |
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