Amino Triazolo Diazepines (Ata) as Constrained Histidine Mimics: IF 6.14

Koen Buysse, Julien Farard, Alexandros Nikolaou, Patrick Vanderheyden, Georges Vauquelin, Daniel Sejer Pedersen, Dirk Tourwe, Steven Ballet

Onderzoeksoutput: Articlepeer review

36 Citaten (Scopus)


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.
Originele taal-2English
Pagina's (van-tot)6468-6471
Aantal pagina's4
TijdschriftOrganic Letters
Nummer van het tijdschrift24
StatusPublished - dec 2012


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