Design,synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole |
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| Authors: | Ohwada Jun Tsukazaki Masao Hayase Tadakatsu Oikawa Nobuhiro Isshiki Yoshiaki Fukuda Hiroshi Mizuguchi Eisaku Sakaitani Masahiro Shiratori Yasuhiko Yamazaki Toshikazu Ichihara Shigeyasu Umeda Isao Shimma Nobuo |
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| Affiliation: | Department of Chemistry, Nippon Roche Research Center, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan. |
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| Abstract: | A highly potent water soluble triazole antifungal prodrug, RO0098557 (1), has been identified from its parent, the novel antifungal agent RO0094815 (2). The prodrug includes a triazolium salt linked to an aminocarboxyl moiety, which undergoes enzymatic activation followed by spontaneous chemical degradation to release 2. Prodrug 1 showed high chemical stability and water solubility and exhibited strong antifungal activity against systemic candidiasis and aspergillosis as well as pulmonary aspergillosis in rats. |
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