期刊
ARCHIVES OF PHARMACAL RESEARCH
卷 40, 期 4, 页码 469-479出版社
PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-017-0886-1
关键词
2-Benzylbenzimidazole; LPS; NF-kappa B inhibitor
资金
- Priority Research Centre Program through the National Research Foundation of Korea (NRF) - Ministry of Education, Science and Technology [2009-0093815]
A novel series of 2-benzylbenzimidazole analogs was designed, synthesized and investigated for their in vitro activities against LPS induced NF-kappa B inhibition in RAW 264.7 cells using the SEAP assay. Among them, 4-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6e, > 100% inhibition at 30 mu M, IC50 = 3.0 mu M), 4-((5-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6j, 96% inhibition at 30 mu M, IC50 = 4.0 mu M) and 2-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6k, 95% inhibition at 30 mu M, IC50 = 5.0 mu M) showed strong inhibitory activity. The structure activity relationship confirmed that the substitution on benzimidazole ring A with hydrophobic cyclohexylmethoxy group at position 4 or 5 markedly enhances the activity. In addition, the hydrophilic hydrogen bonding donor group (OH) at position 2 or 4 on phenyl ring B connected with one methylene spacer to the benzimidazole ring is favorable for the inhibitory activity. However, hydrophobic (-OCH3 and -Cl) groups on phenyl ring B decrease the activity.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据