Studies on antifungal agents. Novel cis-5-alkyl (or alkenyl)-3-phenyl-3-(1H-azol-1-ylmethyl)-2-methyl-isoxazolidine derivatives.
The preparation and in vitro antifungal activity of a novel series of cis-5-alkyl (or alkenyl)-3-phenyl-3-(1H-azol-1-ylmethyl)-2-methylisoxazol idines are described. The overall activity of the 3-(1H-imidazol-1-ylmethyl) analogues was higher than that of the corresponding 3-(1H-1,2,4-triazol-1-ylmethyl) derivatives. Compound 4b emerged as the most potent derivative. When compared to ketoconazole, several of the analogues tested demonstrated equipotent or superior activity against Trichophyton and Candida sp.
Bennett
G A
GA
Department of Organic Chemistry, Fisons Pharmaceuticals, Rochester, NY.
Swift
P A
PA
Mullen
G B
GB
Mitchell
J T
JT
Allen
S D
SD
Georgiev
V S
VS
D000935:Antifungal Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D005658:Fungi / Q000187:drug effects*; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000138:chemical synthesis*
D000935:Antifungal Agents; D007555:Isoxazoles; D010080:Oxazoles