4-烷基-6-芳基-1,3-噻嗪的合成与生物活性有机化学.pdfVIP

DOI: 10.6023/cjoc201212026 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 4-烷基-6-芳基-1,3-噻嗪的合成与生物活性 李 婉a 胡艾希*,a 刘艾林*,b 彭俊梅a 夏 林a 谭卫清a a ( 湖南大学化学化工学院 长沙 410082) (b 中国医学科学院药物研究所 北京 100050) 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 40 μg/mL 浓度下对神经氨酸酶的抑制率达 68.91%, 10 μg/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%. 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 Synthesis and Biological Activities of 4-Alkyl-6-aryl-1,3-thiazines Li, Wana Hu, Aixi*,a Liu, Ailin*,b Peng, Junmei a Xia, Lina Tan, Weiqinga a ( College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082) b ( Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050) Abstract A series of 1,3-thiazine derivatives 1a～1p 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 1i 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 1d, 1e and 1f exhibit good serotonin reuptake inhibitory