< Back to previous page
Publication
Amino Triazolo Diazepines (Ata) as Constrained Histidine Mimics
Journal Contribution - Journal Article
Subtitle:IF 6.14
Abstract: Two synthetic routes for the synthesis of amino-triazolodiazepine (Ata) scaffolds are presented. The scope of both of these proceeding through key intra- and intermolecular Huisgen cycloaddition reactions is discussed. The replacement of the His-Pro dipeptide segment in angiotensin IV by the dipeptide mimetic Ata-Gly and subsequent biological evaluation in two inhibitory enzyme assays validated the use of the Ata moiety as a His mimic given the equipotency of both peptidic analogs.
Journal: Org.Lett.
ISSN: 1523-7060
Issue: 24
Volume: 13
Pages: 6468-6471
Publication year:2012
Keywords:CLICK CHEMISTRY; SIDE-CHAIN; CHI-SPACE; ANALOGS, PEPTIDOMIMETICS; CYCLOADDITION; PEPTIDES; AZIDE, ACID; MIMETICS