Translations:Discovery and development of angiotensin receptor blockers/27/en

Using a different lead, optimization from S-8308, eprosartan was developed by SmithKline Beecham in 1992. Eprosartan does not have a biphenyl-methyl structure but in order to mimic the C-terminal end of Ang II the 5-acetic acid group was replaced with an a-thienylacrylic acid and a 4-carboxy-moiety. Eprosartan is a selective, potent and competitive AT₁ antagonist and its binding to AT₁ receptors is rapid, reversible, saturable and of high affinity.