N－甲基－N－（α－取代萘甲基）取代苄胺类化合物的合成及抗真菌活性

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

报道２５个Ｎ－甲基－Ｎ－（α－取代萘甲基）取代苄胺类化合物的合成及抗真菌活性。抑菌测试结果表明，目标化合物对于８种试验菌种均有不同程度的抑菌活性，化合物６，７，８，１０，１１和２１等活性为ｎａｆｔｉｆｉｎｅ的４～２０倍，化合物８，１０，１１和２１等活性为ｂｕｔｅｎａｆｉｎｅ的２～１０倍，化合物８，９，１０，１１和２１等对Ｓｐｏｒｏｔｒｉｃｈｕｍｓｃｈｅｎｃｋｉｉ及Ａｓｐｅｒｇｉｌｌｕｓｆｕｍｉｇａｔｕｓ的活性为ｃｌｏｔｒｉｍａｚｏｌｅ的８～１５倍，化合物７，８，９和２１等对Ｃｒｙｐｔｏｃｃｏｃｕｓｎｅｏｆｏｒｍａｎｓ亦表现出较高活性，ＭＩＣ为０．３１～１．２５μｇ·ｍｌ－１。

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