Synthesis and evaluation of isoleucine derived angiotensin II AT2 receptor ligands

Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT2R ligand, were designed, synthesized and evaluated for their affinity to the AT2R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, Ki = 8.5 μM) was over 12-times more potent than the lead compound 2.