10种吩嗪衍生物相对于氯法齐明的促氧化活性。
Prooxidative activities of 10 phenazine derivatives relative to that of clofazimine.
作者信息
Zeis B M, Anderson R, O'Sullivan J F
出版信息
Antimicrob Agents Chemother. 1987 May;31(5):789-93. doi: 10.1128/AAC.31.5.789.
Abstract
The objective of this study was to investigate the relationship between the antimycobacterial properties of the antileprosy drug clofazimine and its stimulatory effect on the release of reactive oxidants by polymorphonuclear leukocytes by using a variety of phenazine derivatives. The effects of these compounds on myeloperoxidase-mediated iodination, luminol-enhanced chemiluminescence, and the release of superoxide anion by polymorphonuclear leukocytes were investigated. Dissociation of the antimycobacterial and prooxidative effects of clofazimine was possible by manipulation of the chemical group in position 2 of the phenazine molecule. When nitrogen-containing substituents in this position were replaced by oxygen, the mode of the prooxidative action of the compounds was altered.
摘要
本研究的目的是通过使用多种吩嗪衍生物，研究抗麻风病药物氯法齐明的抗分枝杆菌特性与其对多形核白细胞释放活性氧化剂的刺激作用之间的关系。研究了这些化合物对髓过氧化物酶介导的碘化、鲁米诺增强的化学发光以及多形核白细胞释放超氧阴离子的影响。通过操纵吩嗪分子2位的化学基团，可以使氯法齐明的抗分枝杆菌作用和促氧化作用解离。当该位置的含氮取代基被氧取代时，化合物的促氧化作用模式发生改变。
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