Thiophene congeners of morpholine and allylamine type antifungals--syntheses and biological activities.
A thiophene analogue 8 of the antifungal drug amorolfine (1) was prepared starting from the alcohol 5. In addition, congeners of naftifine, terbinafine and butenafine, in which the naphthalene ring is replaced by a branched thienylalkyl group, wee synthesized. Of the four drug analogues only compound 9, related to terbinafine, showed significant antifungal activity.
Bracher
F
F
Institut für Pharmazeutische Chemie, Technische Universität Braunschweig.
Papke
T
T
D000588:Amines / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D009025:Morpholines / Q000138:chemical synthesis* / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000588:Amines; D000935:Antifungal Agents; D009025:Morpholines; D013876:Thiophenes