Design, synthesis and biological activity of 4 '-[(benzimidazol-1-yl)methyl]biphenyl-2-sulphonamides as dual angiotensin II and endothelin A receptor antagonists

作者：Hao, Li-Ping; Xue, Wei-Zhe; Han, Xiao-Feng; He, Xing; Zhang, Jun; Zhou, Zhi-Ming^*

来源：Medchemcomm, 2015, 6(4): 715-718.

DOI：10.1039/c4md00499j

• 6-SUBSTITUTED AMINOCARBONYL
• BIPHENYLSULFONAMIDES
• BENZIMIDAZOLES
• HYPERTENSION
• DERIVATIVES
• DISCOVERY

A series of novel 4'-[(benzimidazol-1-yl)methyl]biphenyl-2-sulphonamides was designed, and their molecular model simulation fitting to a new HipHop 3D pharmacophore model was examined. Several compounds showed significantly high simulation fit values. The designed compounds were synthesised, 22 of which were biologically evaluated in vitro using the dual receptor binding assay. Compound 11 showed potent antagonistic activity against both angiotensin II AT(1) and endothelin ETA receptors. Obtaining a highly active compound from a candidate set of only 22 compounds illustrates the power and utility of our pharmacophore model.

• 出版日期2015
• 单位北京理工大学