Walker K A, Hirschfeld D R, Marx M
J Med Chem. 1978 Dec;21(12):1335-8. doi: 10.1021/jm00210a037.
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.
描述了1-[2-羟基（巯基）-2-苯乙基]-1-H-咪唑的羧酸酯和（硫）碳酸酯的合成，其中一些通过用酯键取代醚与咪康唑及其类似物存在形式上的关联。在抗真菌生物测定中，许多化合物在体外显示出活性，少数情况下在体内也显示出与咪康唑相当的活性。在该系列中，相对较窄范围内的亲脂性被证明是体外尤其是体内抗真菌活性的必要条件，尽管不是充分条件。
