科研成果
| 论文编号: | DOI:10.1016/j.bmc.2008.10.040 |
| 第一作者所在部门: | 天然产物研究中心 |
| 论文题目: | Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring |
| 作者: | 郭兴洲 |
| 全部作者: | Xing-Zhou Guo,Lin Shi,Rui Wang,Xiao-Xiao Liu, Bo-Gang Li,Xiao-Xia Lu |
| 论文出处: | |
| 刊物名称: | Bioorganic & Medicinal Chemistry |
| 年: | 2008 |
| 卷: | 16 |
| 期: | 24 |
| 页: | 10301-10310 |
| 联系作者: | 卢晓霞 |
| 收录类别: | |
| 影响因子: | 3.075 |
| 摘要 : | A series of benzimidazole derivatives bearing a heterocyclic ring imidazole (1), 5-chloroimidazole (2),1,2,4-triazol (3), and imidazoline (4) were synthesized and evaluated for angiotensin II antagonistic activities.The synthetic compounds 1–4 were biologically evaluated in vitro using an AT1 receptor binding assay, where compounds 1 and 3 provided weak binding affinity, compound 2 showed moderate binding affinity, and compound 4 showed good binding affinity. Moreover, compound 4 was found to be almost equipotent with telmisartan in vivo biological evaluation study. |
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