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Monday 07 October 2002

Synthesis of novel water soluble benzylazolium prodrugs of lipophilic azole antifungals.

By: Ohwada J, Murasaki C, Yamazaki T, Ichihara S, Umeda I, Shimma N.

Bioorg Med Chem Lett 2002 Oct 7;12(19):2775-80

Water soluble N-benzyltriazolium or N-benzylimidazolium salt type prodrugs of several highly lipophilic triazole or imidazole antifungals have been synthesized. They were designed to undergo an enzymatic activation followed by a self-cleavage to release a parent drug. The prodrugs such as 16 had enough chemical stability and water solubility for parenteral use and were rapidly and quantitatively converted to the active substance in human plasma.

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