Translations:Discovery and development of angiotensin receptor blockers/36/en

Pharmacophore and structure-activity relationship

Pharmacophore
There are three functional groups that are the most important parts for the bioactivity of ARBs, see figure 1 for details.
The first one is the imidazole ring that binds to amino acids in helix 7 (Asn²⁹⁵). The second group is the biphenyl-methyl group that binds to amino acids in both helices 6 and 7 (Phe³⁰¹, Phe³⁰⁰, Trp²⁵³ and His²⁵⁶). The third one is the tetrazole group that interacts with amino acids in helices 4 and 5 (Arg¹⁶⁷ and Lys¹⁹⁹).
The tetrazole group has been successfully replaced by a carboxylic acid group as is the case with telmisartan.