水杨酰苯胺二乙基磷酸酯：合成、抗菌活性及细胞毒性
Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity.
作者信息
Vinšová Jarmila, Kozic Ján, Krátký Martin, Stolaříková Jiřina, Mandíková Jana, Trejtnar František, Buchta Vladimír
机构信息
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
出版信息
Bioorg Med Chem. 2014 Jan 15;22(2):728-37. doi: 10.1016/j.bmc.2013.12.016. Epub 2013 Dec 12.
A series of 27 salicylanilide diethyl phosphates was prepared as a part of our on-going search for new antimicrobial active drugs. All compounds exhibited in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium strains, with minimum inhibitory concentration (MIC) values of 0.5-62.5μmol/L. Selected salicylanilide diethyl phosphates also inhibit multidrug-resistant tuberculous strains at the concentration of 1μmol/L. Salicylanilide diethyl phosphates also exhibited mostly the activity against Gram-positive bacteria (MICs ≥1.95μmol/L), whereas their antifungal activity is significantly lower. The IC50 values for Hep G2 cells were within the range of 1.56-33.82μmol/L, but there is no direct correlation with MICs for mycobacteria.
作为我们正在进行的寻找新型抗菌活性药物工作的一部分，制备了一系列27种水杨酰苯胺二乙基磷酸酯。所有化合物均表现出对结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌菌株的体外活性，最低抑菌浓度（MIC）值为0.5 - 62.5μmol/L。所选的水杨酰苯胺二乙基磷酸酯在1μmol/L的浓度下也能抑制耐多药结核菌株。水杨酰苯胺二乙基磷酸酯对革兰氏阳性菌大多也有活性（MIC≥1.95μmol/L），而它们的抗真菌活性则显著较低。对Hep G2细胞的IC50值在1.56 - 33.82μmol/L范围内，但与分枝杆菌的MIC值没有直接相关性。
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