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新型利尿剂依托唑啉的构效关系(作者译)

[Structure-activity relationships of etozolin, a novel diuretic (author's transl)].

作者信息

Satzinger G

出版信息

Arzneimittelforschung. 1977;27(9a):1742-45.

PMID:578762
Abstract

Selection of a structurally confined group of diuretics out of 2-methylenethiazolidones-(4), a new class of compounds, and related heterocycles with partly choleretic properties is described. The physico-chemical parameters of ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetate (3; etozolin, Gö 687, Elkapin), which has been selected for therapeutic use, are discussed with respect to its close structural relation to the choleretic piprozoline (2). Both the spectroscopic results and the anomalous thermodynamic data of 2, 3 and the homologous compounds 4 and 5 demonstrate a structural specificity of 3 unknown up to now with diuretics.

摘要

从一类新型化合物2-亚甲基噻唑烷酮-(4)及具有部分利胆特性的相关杂环化合物中筛选出一组结构受限的利尿剂。已被选作治疗用途的乙酸乙酯(Z)-(3-甲基-4-氧代-5-哌啶基-噻唑烷-2-亚基)酯(3;依托唑啉,Gö 687,埃尔卡平),就其与利胆药匹普唑啉(2)的紧密结构关系进行了讨论。2、3以及同系化合物4和5的光谱结果和异常热力学数据均表明,3具有一种迄今为止利尿剂中未知的结构特异性。

相似文献

1
[Structure-activity relationships of etozolin, a novel diuretic (author's transl)].新型利尿剂依托唑啉的构效关系(作者译)
Arzneimittelforschung. 1977;27(9a):1742-45.
2
[On the pharmacology of Etozolin (author's transl)].关于依托唑啉的药理学(作者译)
Arzneimittelforschung. 1977;27(9a):1745-54.
3
[Comparative studies on the diuretic activities of Etozolin and a reference compound in normal volunteers (author's transl)].依托唑啉与一种对照化合物对正常志愿者利尿活性的比较研究(作者译)
Arzneimittelforschung. 1977;27(9a):1814-7.
4
[Effect of the diuretic Etozolin (Gö 687) on renal elimination of water and solutes in subjects with normal renal function (author's transl)].
Arzneimittelforschung. 1977;27(9a):1804-6.
5
Assay of etozolin and its main metabolite, ozolinone, in plasma by high performance liquid chromatography.
Arzneimittelforschung. 1980;30(10):1788-90.
6
[Effect of the diuretic Etozolin in patients with normal and impaired renal function (author's transl)].
Arzneimittelforschung. 1977;27(9a):1807-14.
7
[Toxicological studies on Etozolin (author's transl)].依托唑啉的毒理学研究(作者译)
Arzneimittelforschung. 1977;27(9a):1758-67.
8
[On the pharmacology of piprozoline (author's transl)].
Arzneimittelforschung. 1977;27(2b):467-75.
9
[TLC-method for quantitative densitometric determination of piprozoline and its main metabolite using internal standards (author's transl)].[采用内标法定量光密度测定哌唑啉及其主要代谢物的薄层色谱法(作者译)]
Arzneimittelforschung. 1977;27(2b):499-502.
10
Independent of etozolin elimination of kidney function. Single dose experiments in patients with renal insufficiency.依他唑胺的消除与肾功能无关。对肾功能不全患者进行的单剂量实验。
Arzneimittelforschung. 1980;30(10):1791-3.

引用本文的文献

1
Placental transfer of etozolin and ozolinone during the first half of gestation in man.
Eur J Clin Pharmacol. 1982;23(3):253-60. doi: 10.1007/BF00547564.
2
Pharmacodynamics and kinetics of etozolin/ozolinone in hypertensive patients with normal and impaired kidney function.依他唑啉/奥唑啉酮在肾功能正常和受损的高血压患者中的药效学和药代动力学。
Eur J Clin Pharmacol. 1984;26(6):687-93. doi: 10.1007/BF00541926.
3
Clinical pharmacokinetics of some newer diuretics.一些新型利尿剂的临床药代动力学
Clin Pharmacokinet. 1987 Oct;13(4):254-66. doi: 10.2165/00003088-198713040-00003.
4
Effects of ozolinone, a diuretic active metabolite of etozoline, on renal function. II. Localization of tubular site of diuretic action by micropuncture in the rat.依他唑胺的利尿活性代谢产物奥索利酮对肾功能的影响。II. 通过大鼠微穿刺法确定利尿作用的肾小管部位
Naunyn Schmiedebergs Arch Pharmacol. 1978 Oct;304(3):289-96. doi: 10.1007/BF00507971.
5
Effects of ozolinone, a diuretic active metabolite of etozoline, on renal function. I. Clearance studies in dogs.
Naunyn Schmiedebergs Arch Pharmacol. 1978 Oct;304(3):283-7. doi: 10.1007/BF00507970.