Synthesis of new 1-[2-Azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazoles and in vitro evaluation of their antifungal activity.
New 1-[2-azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazole were synthesized by nucleophilic substitution of various tertiary alcohols with azide anion in presence of boron trifluoride-diethyl etherate. Their antifungal activity was evaluated against Candida albicans, Candida glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed.
Chevreuil
Francis
F
EA 921, Laboratoire SONAS, UFR des Sciences Pharmaceutiques et Ingenierie de la Sante, Angers, France.
Landreau
Anne
A
Seraphin
Denis
D
Larcher
Gérald
G
Bouchara
Jean-Philippe
JP
Richomme
Pascal
P
D000438:Alcohols; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001232:Aspergillus fumigatus / Q000187:drug effects; D001386:Azides; D002176:Candida albicans / Q000187:drug effects; D041221:Candida glabrata / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000438:Alcohols; D000935:Antifungal Agents; D001386:Azides; D007093:Imidazoles