Kim K H
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064.
J Pharm Sci. 1991 Oct;80(10):966-70. doi: 10.1002/jps.2600801013.
Quantitative structure-activity relationships of the metabolism of drugs by uridine diphosphate (UDP)-glucuronosyltransferase have been investigated. It is observed that most of the variation in the rate of glucuronidation of phenols, thiols, and some other miscellaneous compounds can be accounted for by the lipophilic property of the molecules. The results are consistent with the previous finding with primary and secondary alcohols, and benzoic acids. The optimum lipophilicity for these compounds undergoing metabolism by UDP-glucuronosyltransferase appears to be a log P of 2.
已对尿苷二磷酸（UDP）-葡糖醛酸基转移酶介导的药物代谢的定量构效关系进行了研究。据观察，酚类、硫醇类及其他一些杂类化合物的葡糖醛酸化速率的大部分变化可由分子的亲脂性来解释。这些结果与先前关于伯醇、仲醇和苯甲酸的研究结果一致。这些经UDP-葡糖醛酸基转移酶代谢的化合物的最佳亲脂性似乎是log P为2。
