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 information provided guidance for the further development of endoperoxide and epoxy-endoperoxides as topical antifungal agents.
Avery
Thomas D
TD
Department of Chemistry, The University of Adelaide, 5005 SA, Australia.
Macreadie
Peter I
PI
Greatrex
Ben W
BW
Robinson
Tony V
TV
Taylor
Dennis K
DK
Macreadie
Ian G
IG
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D002176:Candida albicans / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D006224:Cricetinae; D015195:Drug Design; D004912:Erythrocytes / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D010545:Peroxides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D010545:Peroxides