抗结核药物的定向开发（第二部分）：卤代3-(4-烷基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮

The oriented development of antituberculotics (Part II): halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones.

作者信息

Waisser Karel, Matyk Josef, Divisová Hana, Husáková Petra, Kunes Jirí, Klimesová Vera, Palát Karel, Kaustová Jarmila

机构信息

Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovského, Czech Republic.

出版信息

Arch Pharm (Weinheim). 2007 May;340(5):264-7. doi: 10.1002/ardp.200600002.

DOI:10.1002/ardp.200600002

Abstract

Based on our previous studies, 21 new halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones were synthesized by the reaction of salicylanilides and methyl-chloroformate. All compounds were screened in vitro against three different strains of mycobacterium, and Free-Wilson method was used to establish structure-activity relationships. 6-Bromo-3-(4-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione 3b proved to be the most active compound of the series.

摘要

基于我们之前的研究，通过水杨酰苯胺与氯甲酸甲酯反应合成了21种新型卤代3-(4-烷基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮。所有化合物均针对三种不同的分枝杆菌菌株进行了体外筛选，并采用Free-Wilson方法建立构效关系。6-溴-3-(4-丁基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮3b被证明是该系列中活性最高的化合物。

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