本組對於抗血小板凝集的藥物有高度的興趣，我們發現前列腺環素 (PGI2)致效劑中含有1,2,4-oxadiazole雜環具有抗血小板凝集的活性。我們將3-(2-butyric acid-phenyl)-5-phenethyl-[1,2,4]oxadiazole (1a) 當作”線索”化合物，並以雜環(heterocycle)、羧酸基(carboxyl group)、芳香基(aromatic)三個藥理因子為基礎，合成四個系列共44個目標產物來進行藥理活性測試，以期開發具有潛力的抗血小板凝集藥物。

In search of potent anti-platelet compounds, we came across a series of 1,2,4-oxadiazoles with moderate activities. From which, 3-(2-butyric acid-phenyl)-5-phenethyl-[1,2,4]-
oxadiazole (1a) was used as a “lead” for the design and synthesis of better anti-platelet agents. The compound is consisted of three putative pharmacophores: a heterocyclic ring, a carboxyl group and an aromatic moiety. Four series in a total of 44 target compounds have been synthesized and screened for anti-platelet activities. Some of the compounds showed improved activities and will be used as templates for future studies.

中文摘要 I
英文摘要 II
謝誌 III
第一章　緒論
1-1 背景 1
1-2 PGI2致效劑藥理功能 2
1-3 PGI2致效劑與其他衍生物在臨床上的使用 3
1-4 非前類固醇PGI2致效劑 6
1-5 研究動機 10
第二章 合成策略
2-1 反推合成 12
2-2 合成1,2,4-oxadiazole雜環的文獻回顧 13
第三章　實驗結果與討論
3-1 目標產物1a 之合成 15
3-2 雜環(ring B)上，3-苯環(ring A)取代位置的探討 18
3-3 雜環(ring B)上，5-苯環(ring C)與脂肪族取代基之探討 20
3-4 雜環(ring B)上，3-苯環(ring A)取代基之探討 23
3-5 雜環(ring B)上，5-取代(part B)位置與本組其他化合物之研
究 26
第四章　結論
4-1 合成步驟結果 31
4-2 藥理活性結 36
第五章 實驗部份
5-1 本實驗所使用之藥品與儀器 37
5-2 實驗步驟與光譜數據 38
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