title: Studies on antifungal agents. In vitro activity of novel cis-5-alkoxy (or acyloxy)alkyl-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidine derivatives.
abstract: The synthesis and in vitro antifungal activity of a novel series of cis-5-alkoxy(or acyloxy)alkyl-3-phenyl-3-(1H-imidazol-1-ylmethyl)- 2-methylisoxazolidine derivatives (6a-n) are described. The 5-[(4-chlorobenzyloxy)methyl] analogue 6h and the two 5-acyloxymethyl derivatives 6k,l demonstrated the best overall potency. Against Candida stellatoidea, the minimum inhibitory concentrations (MIC's) for 6h,k,l ranged between 0.7 and 2.0 micrograms/ml. The corresponding value for the standard drug ketoconazole was 7-20 micrograms/ml.
authors.affiliation: Department of Organic Chemistry, Fisons Pharmaceuticals, Rochester, NY.
authors.forename: D M
authors.initials: DM
authors.lastname: Maryniak
authors.forename: G B
authors.initials: GB
authors.lastname: Mullen
authors.forename: S D
authors.initials: SD
authors.lastname: Allen
authors.forename: J T
authors.initials: JT
authors.lastname: Mitchell
authors.forename: C R
authors.initials: CR
authors.lastname: Kinsolving
authors.forename: V
authors.initials: V
authors.lastname: St Georgiev
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000138:chemical synthesis*
chemical_list: D000935:Antifungal Agents; D007093:Imidazoles; D007555:Isoxazoles; D010080:Oxazoles