4-烷基-6-芳基-1,3-噻嗪的合成与生物活性  

Synthesis and Biological Activities of 4-Alkyl-6-aryl-1,3-thiazines

作　　者：李婉[1] 胡艾希[1] 刘艾林[2] 彭俊梅[1] 夏林[1] 谭卫清[1] 

机构地区：[1]湖南大学化学化工学院,长沙410082 [2]中国医学科学院药物研究所,北京100050

出　　处：《有机化学》2013年第7期1478-1482,共5页Chinese Journal of Organic Chemistry

基　　金：国家教育部博士点专项基金(No.20040532002)资助项目~~

摘　　要：以芳香醛为原料,经缩合、环化等合成了16种1,3-噻嗪化合物1a～1p,并对其进行了体外神经氨酸酶(NA)和5-羟色胺转运体(SERT)抑制活性测试,测试结果显示部分化合物对神经氨酸酶和5-羟色胺转运体有抑制活性.其中化合物1i在40μg/mL浓度下对神经氨酸酶的抑制率达68.91%,10μg/mL浓度下,1d,1e和1f对5-羟色胺转运体的抑制率分别为99.5%,99.6%和99.8%.A series of 1,3-thiazine derivatives la^lp were designed and synthesized by the reaction of aromatic aldehyde via condensation and cyclization, and their inhibitory activity of nueraminidase （NA） and serotonin reuptake （SERT） were evaluated in vitro. The pharmacological results showed that compound li exhibits good activity of NA with the inhibitory rate of 68.91% at the concentration of 40 μg/mL, which is similar to oseltamivir （inhibitory rate is 72.6%）, moreover, at the con- centration of 10.0 μg/mL, compounds ld, le and If exhibit good serotonin reuptake inhibitory activity with inhibitory rates of 99.5%, 99.6% and 99.8%, respectively.

关 键 词：合成 1 3-噻嗪 神经氨酸酶抑制剂 5-羟色胺转运体抑制剂 

分 类 号：TQ463.5[化学工程—制药化工]