title: Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
abstract: 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 AT(1) and endothelin ET(A) receptors (AT(1) IC(50)=8.5, ET(A) IC(50)=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.
authors: Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
authors: Renren
authors: R
authors: Bai
authors: Zhen
authors: Z
authors: Wei
authors: Jie
authors: J
authors: Liu
authors: Weijia
authors: W
authors: Xie
authors: Hequan
authors: H
authors: Yao
authors: Xiaoming
authors: X
authors: Wu
authors: Jieyun
authors: J
authors: Jiang
authors: Qiujuan
authors: Q
authors: Wang
authors: Jinyi
authors: J
authors: Xu
mesh_terms: D057911:Angiotensin Receptor Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D065130:Endothelin A Receptor Antagonists; D006801:Humans; D008297:Male; D015394:Molecular Structure; D051381:Rats; D011918:Rats, Inbred SHR; D011945:Receptors, Angiotensin / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: C576628:4'-((benzimidazole-1-yl)methyl)biphenyl-2-sulfonamide; D057911:Angiotensin Receptor Antagonists; D001562:Benzimidazoles; D065130:Endothelin A Receptor Antagonists; D011945:Receptors, Angiotensin; D013449:Sulfonamides