Studies on antifungal agents. 19. Effect of the C-5-aromatic substitution on the in vitro activity of novel 3,5-substituted isoxazolidines.
The influence of the C-5-aromatic substitution on the in vitro antifungal activity of novel cis-3,5-substituted isoxazolidine derivatives was investigated. Compounds having a C-5-(substituted phenoxy)methyl group were found to be the most active against Trichophyton rubrum, Aspergillus fumigatus and Candida albicans with MIC values ranging from 0.7 to 70.0 micrograms/ml. Replacing the phenoxymethyl group with either naphthyl or 2-oxo-1,3-benzoxathiol-6-yl groups resulted in a diminished in vitro activity.
Mullen
G B
GB
Department of Organic Chemistry, Pennwalt Corporation, Rochester, N.Y.
Mitchell
J T
JT
Allen
S D
SD
Georgiev
V S
VS
D000935:Antifungal Agents / Q000138:chemical synthesis*; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005658:Fungi / Q000187:drug effects*; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D010080:Oxazoles / Q000138:chemical synthesis*; D014249:Trichophyton / Q000187:drug effects
D000935:Antifungal Agents; D007555:Isoxazoles; D010080:Oxazoles