Synthesis of a New Class of Druglike Angiotensin II C-Terminal Mimics with Affinity for the AT 2 Receptor

ArticleinJournal of Medicinal Chemistry 50(7):1711-5 · May 2007with6 Reads
Impact Factor: 5.45 · DOI: 10.1021/jm0613469 · Source: PubMed

    Abstract

    Four tripeptides corresponding to the C-terminal region of angiotensin II were synthesized. One of these peptides (Ac-His-Pro-Ile) showed moderate binding affinity for the AT2 receptor. Two aromatic histidine-related scaffolds were synthesized and introduced in the tripeptides to give eight new peptidomimetic structures. Three of the new peptide-derived druglike molecules exhibited selective, nanomolar affinity for the AT2 receptor. These ligands may become lead compounds in the future development of novel classes of selective AT2 receptor agonists.