Rakowitz Dietmar, Angerer Helga, Matuszczak Barbara
Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Arch Pharm (Weinheim). 2006 Oct;339(10):547-58. doi: 10.1002/ardp.200600024.
In continuation of our work aimed towards the preparation of novel aldose reductase inhibitors, several O-substituted hydroxyphenylacetic acid derivatives were investigated. The highest inhibitory activity was found for compounds 7b and 7c bearing a cyclohexylmethyl substituent. This result demonstrates that within these series, this moiety is a useful surrogate for the 4-bromo-2-fluorobenzyl residue which can be often found in potent aldose reductase inhibitors.
在我们致力于制备新型醛糖还原酶抑制剂的工作的延续中,研究了几种O-取代的羟基苯乙酸衍生物。发现带有环己基甲基取代基的化合物7b和7c具有最高的抑制活性。这一结果表明,在这些系列中,该部分是4-溴-2-氟苄基残基的有用替代物,4-溴-2-氟苄基残基在有效的醛糖还原酶抑制剂中经常可以找到。