The modulation of the renin-angiotensin system continues to be an impo
rtant target in drug design. The development of nonpeptide angiotensin
II receptor antagonists offers a new tool in treatment of hypertensio
n. Starting from benzimidazole lead structures detailed structure-acti
vity analyses, molecular modeling methods, and dedicated syntheses led
to the development of potent, orally active antihypertensive drugs.