Amino acids (AAs) play an important role in the modern health industry. The aim
of this article was to assess that AAs’ residues are frequently found in the structures of smallmolecule
modern pharmaceuticals, while peptidomimetics and peptide-based drugs are entirely
derived from AAs. Currently, AAs serve as key structural features in numerous successful
pharmaceuticals, so-called blockbuster drugs. In this work, we provide a detailed profile
of 5 peptidomimetics and 4 peptide drugs. For each compound, we describe the spectrum of
biological activity, medicinal chemistry discovery, and synthetic preparation.