抗结核药物的定向开发：水杨酰苯胺类
The oriented development of antituberculotics: salicylanilides.
作者信息
Waisser Karel, Matyk Josef, Divisová Hana, Husáková Petra, Kunes Jirí, Klimesová Vera, Kaustová Jarmila, Möllmann Ute, Dahse Hans-Martin, Miko Milan
机构信息
Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy, Hradec Králové, Czech Republic.
出版信息
Arch Pharm (Weinheim). 2006 Nov;339(11):616-20. doi: 10.1002/ardp.200600093.
On the basis of our previous results 22 salicylanilides were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The Free-Wilson method was used to evaluate structure-antimycobacterial activity relationships. 4-Chloro-N-(4-propylphenyl)salicylamide and 5-chloro-N-(4-propylphenyl)salicylamide were selected for preclinical studies.
基于我们之前的研究结果，合成了22种水杨酰苯胺类化合物。测试了这些化合物对结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌的体外抗分枝杆菌活性。采用Free-Wilson方法评估结构-抗分枝杆菌活性关系。选择4-氯-N-(4-丙基苯基)水杨酰胺和5-氯-N-(4-丙基苯基)水杨酰胺进行临床前研究。
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