合成并表征了5种4,6-二芳基-2-氨基嘧啶类化合物.测试了它们对大肠肝菌甲硫酰胺肽酶(EcMetAP)的抑制作用及对CXCR4受体的拮抗作用.发现5种化合物均对EcMetAP酶活有抑制作用,除化合物2外均对CXCR4受体有拈抗作用.利用Fie|dTemplater和FieldAlign软件对化合物1-5的上述活性构效关系进行了分析,初步认为化合物的嘧啶环3位N原子及4位取代苯环上若引入给电子基团,可增强这类化合物的EcMetAP酶抑制活性;在嘧啶环2位引入负电性较强的基团取代,改造2个苯环和嘧啶环的4、5、6位C原子的结构可增强其CXCR4受体拮抗活性.
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