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ID: ALA3244395

Journal: J Med Chem

Title: Antimycotic imidazoles. 2. Synthesis and antifungal properties of esters of 1-[2-hydroxy(mercapto)-2-phenylethyl]-1H-imidazoles.

Authors: Walker KA, Hirschfeld DR, Marx M.

Abstract: The synthesis of carboxylic and (thio)carbonate esters of 1-[2-hydroxy(mercapto)-2-phenylethyl]-1-H-imidazoles, some of which are formally related to miconazole and its analogues by replacement of an ether with an ester linkage, is described. In antifungal bioassays a number of compounds display in vitro and, in a few cases, in vivo activities comparable to that of miconazole. In this series lipophilicity within a relatively narrow range is shown to be a necessary, although not sufficient, criterion for in vitro and, in particular, in vivo antifungal activity.

CiteXplore: 722748

DOI: 10.1021/jm00210a037