SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF N-METHYL-N-(α-SUBSTITUTED-NAPHTHALENEMETHYL)SUBSTITUTED BENZYLAMINES

Twenty-five N-methyl-N-(α-substituted-naphthalenemethyl)substitutedbenzylamines were synthesized and twenty-four of them are reported for the first time. Results of preliminary biological tests suggested that all title compounds are active against theeight tested fungi to different degrees.The antifungal activities of compounds 6,7,8,10,11 and 21are 4~20 times more active than that of naftifine,Compounds 8,10,11 and 21 are 2~10 times moreactive than butenafine.Compounds 8,9,10, 11 and 21 are 8~15 times more active than clotrimazoleagainst Sporotrichum schenckii and Aspergillus fumigatus, Compounds 7,8,9 and 21 also showedcomparatively high activities against Cryptoccocus neoformans,with MIC from0.31μg · ml^-1 to 1.25μg · ml^-1.