大鼠体内硝基咪唑类和硝基噻唑类药物的亲脂性与尿排泄之间的关系。

Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.

作者信息

Cantelli-Forti G, Guerra M C, Barbaro A M, Hrelia P, Biagi G L, Borea P A

出版信息

J Med Chem. 1986 Apr;29(4):555-61. doi: 10.1021/jm00154a021.

Abstract

Many processes are involved in the renal excretion of drugs, but very little is known about their quantitative structure-activity relationship. The relationship between urinary excretion and lipophilic character of a series of nitroimidazoles and nitrothiazoles was studied. The unmetabolized forms of the drugs were detected in the urine by means of UV and HPLC procedures. The urinary excretion of unmetabolized forms is parabolically related with the log P, as an expression of lipophilic character of molecules.

摘要

药物经肾排泄涉及许多过程，但对其定量构效关系却知之甚少。研究了一系列硝基咪唑和硝基噻唑的尿排泄与亲脂性之间的关系。通过紫外和高效液相色谱法检测尿液中未代谢形式的药物。未代谢形式的尿排泄与作为分子亲脂性指标的log P呈抛物线关系。