| 含磺胺嘧啶结构单元β-氨基酮的合成及其生物活性 |
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| 引用本文： | 唐雪梅,范莉,赵琴,杨大成. 含磺胺嘧啶结构单元β-氨基酮的合成及其生物活性[J]. 应用化学, 2015, 32(11): 1231-1239. DOI: 10.11944/j.issn.1000-0518.2015.11.150070 |
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| 作者姓名： | 唐雪梅 范莉 赵琴 杨大成 |
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| 作者单位： | 西南大学 生命科学学院;西南大学 化学化工学院 重庆 400715 |
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| 基金项目： | 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 |
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| 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%。
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| 关 键 词： | 糖尿病 过氧化物酶体增殖物激活受体反应元件(PPRE) α-葡萄糖苷酶 Mannich反应 β-氨基酮 磺胺嘧啶 |
| 收稿时间： | 2015-02-20 |
Synthesis and Bioactivities of β-Amino Ketones Containing Sulfadiazine Moiety |
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| TANG Xuemei,FAN Li,ZHAO Qin,YANG Dacheng. Synthesis and Bioactivities of β-Amino Ketones Containing Sulfadiazine Moiety[J]. Chinese Journal of Applied Chemistry, 2015, 32(11): 1231-1239. DOI: 10.11944/j.issn.1000-0518.2015.11.150070 |
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| Authors: | TANG Xuemei FAN Li ZHAO Qin YANG Dacheng |
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| Affiliation: | School of Life Science;School of Chemistry and Chemical Engineering,Southwest University,Chongqing 400715,China |
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| Abstract: | 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 by 1H NMR, 13C 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%). |
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| Keywords: | diabetes mellitus peroxisome proliferator-activated receptor response element(PPRE) α-glucosidase Mannich reaction β-amino ketones sulfadiazine |
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