摘要
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 ,1 HNMR ,MS及元素分析确证 ,并通过1 HNMR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 .
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 A 2 receptor antagonist, to give target compounds I 1～I 8, 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 showed that most of these target compounds exhibited potent antiasthmatic activities, among which I 1 and I 2 were more active than control SD.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2004年第6期631-636,共6页
Chinese Journal of Organic Chemistry
