摘要
通过原子经济的Mannich反应实现了磺胺嘧啶、1-萘乙酮与芳香醛三组分的连接,直接合成了16个含有磺胺嘧啶结构单元的未见报道的β-氨基酮;所得化合物经1H NMR、13C NMR、HRMS和MS等技术手段确证其结构。生物活性测试结果显示,在17.04~19.69 nmol/L浓度范围内,所有目标分子的α-葡萄糖苷酶抑制活性很弱,但部分目标分子的过氧化物酶体增殖物激活受体反应元件（PPRE）激动活性较好,最高达到了52%。
Sixteen new β-amino ketones containing sulfadiazine moiety have been directly synthesized through atom-economic Mannich reaction of sulfadiazine with 1-acetonaphthone and some aromatic aldehydes. The chemical structures of these obtained compounds were identified by1 H NMR,13 C NMR,and HRMS. The biological assay results show that all obtained compounds in the concentration range of 17. 04 ~ 19. 69 nmol / L possess very weak α-glucosidase inhibitory activities, while some compounds can activate peroxisome proliferator-activated receptor response element（ PPRE） moderately,of which one exhibits the strongest activity（ 52%）.
出处
《应用化学》
CAS
CSCD
北大核心
2015年第11期1231-1239,共9页
Chinese Journal of Applied Chemistry
基金
中央高校基本业务费专项资金(XDJK2015C128)
重庆市自然科学基金(2005BB5095)资助~~
