Koechel D A, Rankin G O, Sloan W R
J Med Chem. 1979 Jul;22(7):830-4. doi: 10.1021/jm00193a015.
A group of [4-(2-bromoalkanoyl)phenoxy]acetic acids was studied to determine if there was an association between the alkylating ability and the diuretic activity of its members. Acute studies in dogs revealed that there is not a consistent correlation in the alkylating potential of these alpha-bromo ketones and their ability to induce a diuretic response. In addition, pretreatment of dogs with the various alpha-bromo ketones did not alter the diuretic activity normally observed with ethacrynic acid (EA). The role of chemical-induced renal tissue alkylation in the initiation of a diuresis or a nephrotoxic response is discussed.
对一组[4-(2-溴代烷酰基)苯氧基]乙酸进行了研究,以确定其成员的烷基化能力与利尿活性之间是否存在关联。对狗的急性研究表明,这些α-溴代酮的烷基化潜力与其诱导利尿反应的能力之间没有一致的相关性。此外,用各种α-溴代酮对狗进行预处理并没有改变通常观察到的依他尼酸(EA)的利尿活性。本文讨论了化学诱导的肾组织烷基化在利尿或肾毒性反应起始中的作用。