Bracher F, Papke T
Institut für Pharmazeutische Chemie, Technische Universität Braunschweig.
Pharmazie. 1995 Aug;50(8):525-7.
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.
从醇5开始制备了抗真菌药物阿莫罗芬(1)的噻吩类似物8。此外,还合成了萘替芬、特比萘芬和布替萘芬的类似物,其中萘环被支链噻吩基烷基取代。在这四种药物类似物中,只有与特比萘芬相关的化合物9表现出显著的抗真菌活性。