Design of endoperoxides with anti- Candida activity

Broad antifungal structure–activity relationships governing epoxy-endoperoxides 2 and 3 and their parent endoperoxides 1 are reported. Their inhibitory activity against Candida albicans in conjunction with hemolytic activity and/or growth inhibition of cultured mammalian cells are reported. This inf...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2007, Vol.15 (1), p.36-42
Hauptverfasser:	Avery, Thomas D., Macreadie, Peter I., Greatrex, Ben W., Robinson, Tony V., Taylor, Dennis K., Macreadie, Ian G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antifungal Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Artemisinin Candida Candida albicans Candida albicans - drug effects Cell Proliferation - drug effects CHO Cells Cricetinae Drug Design Endoperoxide Erythrocytes - drug effects Growth inhibition Hemolytic activity Humans Microbial Sensitivity Tests Molecular Conformation Peroxides - chemical synthesis Peroxides - chemistry Peroxides - pharmacology Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	Broad antifungal structure–activity relationships governing epoxy-endoperoxides 2 and 3 and their parent endoperoxides 1 are reported. Their inhibitory activity against Candida albicans in conjunction with hemolytic activity and/or growth inhibition of cultured mammalian cells are reported. This information provided guidance for the further development of endoperoxide and epoxy-endoperoxides as topical antifungal agents.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2006.10.021