Literature data published mainly in the last 15 years on the synthesis and biological properties of amino acid analogues and
derivatives containing tetrazolyl moieties are analyzed. Tetrazolyl analogues and derivatives of amino acids and peptides are
shown to be promising for medicinal chemistry. Being polynitrogen heterocyclic systems comprising four endocyclic nitrogen
atoms, tetrazoles can behave as acids and bases and form strong hydrogen bonds with proton donors (more rarely, with
acceptors). They have high metabolic stability and are able to penetrate biological membranes. The review also considers the
synthesis and properties of linear and cyclic peptides based on modified amino acids incorporating a tetrazolyl moiety. A
special issue is the discussion of the biological properties of tetrazole-containing amino acids and peptides, which exhibit high
biological activity and can be used to design new drugs.
The bibliography includes 200 references.