Chinese Journal of Organic Chemistry ›› 2004, Vol. 24 ›› Issue (6): 631-636. Previous Articles     Next Articles

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

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