• YAKHAK HOEJI
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• v.37 no.3
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• pp.247-253
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• 1993

Eight new derivatives of allylamine which are related to naftifine and expected to have antifungal activity were synthesized. Schiff base 2a-2d and 2'e-2'h were obtained by conventional methods using trans-cinnamylamine or trans-cinnamaldehyde. The reduction of azomethine linkage with NaBH$_{4}$ yielded secondary amine 3a-3h, which were then methylated by means of HCHO and excess NaBH$_{4}$ or HCOOH to give 4a-4h.

• YAKHAK HOEJI
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• v.48 no.4
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• pp.254-260
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• 2004

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 2,4-difluorophenyl( 2a-5a), 2,5-difluorophenyl(2b-5b), 4-ethylphenyl(2c-5c), 2-hydroxyphenyl(2d-5d) and 2-methylnaphthyl(2e-5e) instead of naphthyl group with hydrogen(3a-3e), methyl(4a-4e), and ethyl(5a-5e) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds( 3a, 4a, 5a, 3d, 4d, 4d, 5d, 3e, and 4e) showed significant anti-fungal activity against T. mentagroPhytes. (E)-N-(3-Phenyl-2-propenyl)-2- hydroxy-benzenemethaneamine( 3d) displayed moderate antifungal activity against all five different fungi.

• YAKHAK HOEJI
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• v.47 no.5
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• pp.293-299
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• 2003

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 4-fluorophenyl(2a-5a), 2-fluorophenyl(2b-5b), 2,4-dichlorophenyl(2c-5c), 2,6-dichlorophenyl(2d-5d), 4-nitrophenyl(2e-5e), and 2,3-dihydro-benzo[1,4]dioxan-6-yl( 2f-5f) instead of naphthyl group with hydrogen(3a-3f), methyl(4a-4f), and ethyl(5a-5f) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds(3a, 5a, 3c, 4c, 4d, 5d, 5e, and 4f) showed significant antifungal activity against T. mentagrophytes. (E)-N-Ethyl-(3-phenyl-2-propenyl)-4-nitro-benzenemethaneamine(5e) displayed moderate antifungal activity against all five different fungi.