Prooxidative activities of 10 phenazine derivatives relative to that of clofazimine | Zendy

Birgit M. Zeis | Zendy; Ronald Anderson | Zendy; John O’Sullivan | Zendy

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Prooxidative activities of 10 phenazine derivatives relative to that of clofazimine

Author(s) -

Birgit M. Zeis,

Ronald Anderson,

John O’Sullivan

Publication year - 1987

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.31.5.789

Subject(s) - clofazimine , phenazine , superoxide , chemistry , myeloperoxidase , antimycobacterial , plumbagin , luminol , reactive oxygen species , chemiluminescence , biochemistry , pharmacology , organic chemistry , biology , enzyme , medicine , immunology , inflammation , mycobacterium tuberculosis , tuberculosis , leprosy , pathology , genetics

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.

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