575465-30-4Relevant academic research and scientific papers
Synthesis and biological evaluation of 4′-[(benzimidazole-1-yl) methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists
Bai, Renren,Wei, Zhen,Liu, Jie,Xie, Weijia,Yao, Hequan,Wu, Xiaoming,Jiang, Jieyun,Wang, Qiujuan,Xu, Jinyi
experimental part, p. 4661 - 4667 (2012/09/07)
A series of 4′-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50 = 8.5, ETA IC50 = 8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure-activity relationships were also discussed in the present paper.
Design, synthesis, and biological evaluation, of the first selective nonpeptide AT2 receptor agonist
Wan, Yiqian,Wallinder, Charlotta,Plouffe, Bianca,Beaudry, Hélène,Mahalingam,Wu, Xiongyu,Johansson, Berndt,Holm, Mathias,Botoros, Milad,Karlén, Anders,Pettersson, Anders,Nyberg, Fred,F?ndriks, Lars,Gallo-Payet, Nicole,Hallberg, Anders,Alterman, Mathias
, p. 5995 - 6008 (2007/10/03)
The first druglike selective angiotensin II AT2 receptor agonist (21) with a Ki value of 0.4 nM for the AT2 receptor and a Ki > 10 μM for the AT1 receptor is reported. Compound 21, with a bioavailability of 20-3
