[以氯噻嗪和异戊巴比妥为例的药物硫代类似物的合成、结构解析及生物活性]

[Synthesis, structure elucidation and biological activity of thio- analogs of drugs with the examples of chlorthenoxazine and amobarbital].

作者信息

Stratmann J

机构信息

Institut für Pharmazie, Johannes Gutenberg-Universität Mainz.

出版信息

Pharmazie. 1990 Sep;45(9):668-70.

Abstract

Two drugs (chlorthenoxazine, amobarbital) were converted into their S-analogues derivatives via thiation with the P4S10-pyridine complex. The identity of structure isomers was confirmed by 13C NMR. A preliminary evaluation for their biological activities revealed that trithioamobarbital exhibits some notable spasmolytic effects. The substitution of oxygen by sulphur in chlorthenoxazine resulted in a complete loss of antiinflammatory activity.

摘要

通过与P4S10 - 吡啶络合物进行硫代反应，将两种药物（氯西诺嗪、异戊巴比妥）转化为它们的S - 类似物衍生物。通过13C NMR确认了结构异构体的身份。对其生物活性的初步评估表明，三硫代异戊巴比妥表现出一些显著的解痉作用。氯西诺嗪中氧被硫取代导致抗炎活性完全丧失。

相似文献

1

[Synthesis, structure elucidation and biological activity of thio- analogs of drugs with the examples of chlorthenoxazine and amobarbital].[以氯噻嗪和异戊巴比妥为例的药物硫代类似物的合成、结构解析及生物活性]

Pharmazie. 1990 Sep;45(9):668-70.

2

3-Aroylmethyl-2H-1,3-benzoxazinedione derivatives with anticholinergic and antihistaminic activities.

Farmaco. 1993 Jul;48(7):1015-20.

3

New 1,3-benzoxazin-2-ones or thiones of molluscacidal activity.具有杀软体动物活性的新型1,3-苯并恶嗪-2-酮或硫酮。

Pharmazie. 2000 Jun;55(6):426-8.

4

[Pyridinol derivatives (4). Synthesis and pharmacological actions of 3,4-dihydro-2H-pyrido[3,2-b]-1,4-oxazine derivatives. (1)].[吡啶醇衍生物（4）。3,4-二氢-2H-吡啶并[3,2-b]-1,4-恶嗪衍生物的合成及药理作用。（1）]

Yakugaku Zasshi. 1983 May;103(5):497-507.

5

[Research on 2,3-benzoxazines. XVI (1). Synthesis of 4-methyl-and 1-methyl-3,4-dihydro-1H-2,3-benzoxazines and derivatives].[2,3-苯并恶嗪的研究。十六（1）。4-甲基和1-甲基-3,4-二氢-1H-2,3-苯并恶嗪及其衍生物的合成]

Farmaco Sci. 1972 Jan;27(1):30-45.

6

Substituted thiazolidinediones and thio-imidazolidinones: synthesis, structural study and pharmacological activity.取代噻唑烷二酮类和硫代咪唑烷酮类：合成、结构研究及药理活性。

Pharmazie. 1995 Jun;50(6):387-9.

7

Tricyclic heteroaromatic systems. 2-Phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one: a novel benzodiazepine receptor ligand.三环杂芳族体系。2-苯基-1,2,4-三唑并[1,5-c][1,3]苯并恶嗪-5-酮：一种新型苯二氮卓受体配体。

Farmaco. 1994 Feb;49(2):89-92.

8

[3-Dialkylamino-substituted 2H-1,4-benzoxazines].[3-二烷基氨基取代的2H-1,4-苯并恶嗪]

Farmaco Sci. 1986 Dec;41(12):942-53.

9

N-arylpiperazinyl derivatives of 2,3-dihydrobenzoxazin[1,4]-3-ones synthesis and normolipemic activity.2,3-二氢苯并恶嗪[1,4]-3-酮的N-芳基哌嗪基衍生物的合成及降血脂活性

Farmaco. 1993 Aug;48(8):1079-89.

10

Research on heterocyclic compounds. XXXVIII. Synthesis and pharmacological activity of imidazo[1,2-b]pyridazine-2-carboxylic derivatives.杂环化合物的研究。三十八。咪唑并[1,2 - b]哒嗪 - 2 - 羧酸衍生物的合成及药理活性

Farmaco. 1997 Apr;52(4):213-7.

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验