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有机化学
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有机化学 ›› 2004, Vol. 24 ›› Issue (6): 631-636. 上一篇    下一篇

研究论文

塞曲司特衍生物的合成和抗哮喘活性

张治国a, 张奕华*,a, 季晖b, 邱苏赣b   

  1. a中国药科大学新药研究中心 南京 210009
    b中国药科大学药理学教研室 南京 210009
  • 收稿日期:2003-09-08 修回日期:2003-10-27 接受日期:2003-12-15 发布日期:2022-09-21
  • 通讯作者: *E-mail: zyhtgd@hotmail.com

Synthesis and Antiasthmatic Activity of Seratrodast Derivatives

ZHANG, Zhi-Guoa, ZHANG, Yi-Hua*,a, JI, Huib, QIU,Su-Ganb   

  1. a Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009
    b Department of Pharmacology, China Pharmaceutical University, Nanjing 210009
  • Received:2003-09-08 Revised:2003-10-27 Accepted:2003-12-15 Published:2022-09-21

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合成了8个2,4-二芳基-1,3-二氧戊环、-1,3-二硫戊环及2,5-二芳基-1,3-氧硫戊环胺类化合物,将其分别与血栓素A2(TXA2)受体拮抗剂塞曲司特(Seratrodast, SD)进行酰化反应,制备了目标化合物I1～I8,结构经IR, 1H NMR, MS及元素分析确证,并通过1H NMR鉴别产物顺反异构体的存在及其相应比例.初步药理试验表明,绝大多数目标物都具有较高的抗哮喘活性,其中I1, I2的抗哮喘活性高于阳性对照药SD.

关键词: 血栓素A2受体拮抗剂, 塞曲司特, 合成, 抗哮喘活性

Eight 2,4-diaryl-1,3-dioxolane, -1,3-dithiolane and 2,5-diaryl-1,3-oxothiolane amino compounds were synthesized, which were then acylated through seratrodast (SD), a thromboxane A2 receptor-antagonist, to givetarget compounds I1～I8, and their structures were confirmed by IR, 1H NMR,MS and elemental analysis. The existence and ratio of cis- to trans-isomers were identified by 1H NMR. Preliminary pharmacological test showedthat most of these target compounds exhibited potent antiasthmatic activities, among which I1 and I2 were more active than control SD.

Key words: thromboxane A2 receptor-antagonist, seratrodast,synthesis, antiasthmatic activity