- 作者: 陳清玉,葉忍莉,陳玉霖,簡偉明*
- 作者服務機構: Department of Pharmacology, National Cheng Kung University, Tainan 70101, Taiwan, R.O.C.
- 中文摘要:
Prostacyclin is involved in many pathological conditions, such as sensitization of inflammation induced
pain and isovolumetic distention. Therefore, antagonism of prostacyclin action may be useful in the
alleviation of these conditions. In this study, novel potent prostacyclin antagonists, 2-[4-(imidazolin-2-
ylideneamino)benzyl]-indan-1-ones were synthesized from their respective substituted indanones in three
steps. The construction of the amino-imidazole moiety of these derivatives is achieved by using in situ
generation of chloro-imidazole and reaction with their respective anilines. Thus, these N-substituted 2-
imidazolines can be prepared safely and efficiently.Moreover, these compounds show potent prostacyclin
antagonistic activity by inhibition of prostacyclin agonist induced ERK1/2 phosphorylation in human
erythroleukemia cells.Moreover, we observed an increase in activity with the increase in electro-donating
property of the substitution on the indanone aromatic ring. Prostacyclin antagonists with increased potency
may be designed based on these findings. These compounds may also be invaluable tools for the
study of the physiological functions of prostacyclin. - 英文摘要: --
- 中文關鍵字: Prostacyclin antagonist; Imidazolines.
- 英文關鍵字: --