338990-34-4Relevant academic research and scientific papers
N-substituted carbamoyloxyalkyl-azolium derivatives
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Page/Page column 36-37, (2010/02/09)
N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
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
, p. 191 - 196 (2007/10/03)
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.
