Translations:Discovery and development of angiotensin receptor blockers/22/en

Research investigators at Takeda discovered in 1982 the weak nonpeptide Ang II antagonists S-8307 and S-8308 from a group of 1-benzylimidazole-5-acetic acid derivatives. S-8307 and S-8308 have moderate potency, short duration of action and limited oral bioavailability, however they are selective and competitive AT₁ receptor antagonists without partial agonist activity. A group at DuPont postulated that both Ang II and the Takeda leads were bound at the same receptor site. These two substances served as lead compounds for further optimization of AT₁ receptor blockers.