所选吩嗪类化合物对体外麻风分枝杆菌的构效关系
Structure-activity relationships of selected phenazines against Mycobacterium leprae in vitro.
作者信息
Franzblau S G, O'Sullivan J F
机构信息
Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
出版信息
Antimicrob Agents Chemother. 1988 Oct;32(10):1583-5. doi: 10.1128/AAC.32.10.1583.
Abstract
Structure-activity relationships of phenazines against Mycobacterium leprae were investigated by using an in vitro radiorespirometric assay. In general, activity in ascending order was observed in compounds containing no chlorine atoms, a monochlorinated phenazine nucleus, and chlorines in the para positions of both the anilino and phenyl rings. The most active compounds contained a 2,2,6,6-tetramethylpiperidine substitution at the imino nitrogen. Most of these chlorinated phenazines were considerably more active in vitro than clofazimine (B663).
摘要
通过体外放射性呼吸测定法研究了吩嗪对麻风分枝杆菌的构效关系。一般来说，在不含氯原子的化合物、单氯代吩嗪核以及苯胺基环和苯环对位均含氯的化合物中观察到活性呈升序排列。活性最高的化合物在亚氨基氮处含有2,2,6,6 - 四甲基哌啶取代基。这些氯化吩嗪中的大多数在体外比氯法齐明（B663）活性高得多。
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