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Communication | Special issue | Vol 82, No. 1, 2010, pp.289-295
Published online, 9th July, 2010
DOI: 10.3987/COM-10-S(E)55
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 University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan


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.