Franzblau S G, White K E, O'Sullivan J F
Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
Antimicrob Agents Chemother. 1989 Nov;33(11):2004-5. doi: 10.1128/AAC.33.11.2004.
In a previous study of structure-activity relationships of selected phenazines against Mycobacterium leprae in vitro, compounds containing a 2,2,6,6-tetramethylpiperidine substitution at the imino nitrogen were most active. Therefore, the effect of substitution at the para positions of the phenyl and anilino groups in tetramethylpiperidine-substituted phenazines was assessed. As determined by radiorespirometry, activity in ascending order was observed in compounds substituted with hydrogens or fluorines, ethoxy groups, methyl groups, chlorines, and bromines and correlated with partition coefficients in octanol-water.
在先前一项关于所选吩嗪类化合物体外抗麻风分枝杆菌构效关系的研究中，在亚氨基氮处含有2,2,6,6 - 四甲基哌啶取代基的化合物活性最高。因此，评估了四甲基哌啶取代的吩嗪类化合物中苯基和苯胺基对位取代的影响。通过放射性呼吸测定法确定，用氢或氟、乙氧基、甲基、氯和溴取代的化合物活性呈升序排列，且与正辛醇 - 水分配系数相关。
