Author/Authors :
Jun Ohwada، نويسنده , , Masao Tsukazaki، نويسنده , , Tadakatsu Hayase، نويسنده , , Nobuhiro Oikawa، نويسنده , , Yoshiaki Isshiki، نويسنده , , Hiroshi Fukuda، نويسنده , , Eisaku Mizuguchi، نويسنده , , Masahiro Sakaitani، نويسنده , , Yasuhiko Shiratori، نويسنده , , Toshikazu Yamazaki، نويسنده , , Shigeyasu Ichihara، نويسنده , , Isao Umeda، نويسنده , , Nobuo Shimma، نويسنده ,
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.
