Antifungal sordarins. part 3: synthesis and structure-activity relationships of 2',3'-fused oxirane derivatives.
A number of new 2',3'-fused oxirane derivatives were synthesized for structure-activity relationship study. Many of these derivatives exhibit high potency against Candida spp. In addition, sordarin manno epoxide derivative 6 presents in vivo therapeutic effect in mice and is considered a promising antifungal lead within this series.
Castro
Julia
J
GlaxoSmithKline, Research Department, Parque Tecnológico de Madrid, Severo Ochoa, 2. 28760 Tres Cantos, Madrid, Spain.
Cuevas
Juan C
JC
Fiandor
José M
JM
Fraile
Ma Teresa
MT
de las Heras
Federico Gómez
FG
Ruiz
José R
JR
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D002175:Candida / Q000187:drug effects*; D015195:Drug Design; D004852:Epoxy Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005027:Ethylene Oxide / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007192:Indenes; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D004852:Epoxy Compounds; D007192:Indenes; C003329:sordarin; D005027:Ethylene Oxide