title: Synthesis of dehydrodipeptide esters and their evaluation as inhibitors of cathepsin C.
abstract: The procedures for the synthesis of esters of dehydropeptides containing C-terminal (Z)-dehydrophenylalanine and dehydroalanine have been elaborated. These esters appeared to be moderate or weak inhibitors of cathepsin C, with some of them exhibiting slow-binding behavior. As shown by molecular modeling, they are rather bound at the surface of the enzyme and are not submersed in its binding cavities.
authors.affiliation: Faculty of Chemistry, Opole University, Oleska 48, 45-052 Opole, Poland.
authors.forename: Maciej
authors.initials: M
authors.lastname: Makowski
authors.affiliation: Faculty of Chemistry, Opole University, Oleska 48, 45-052 Opole, Poland.
authors.forename: Paweł
authors.initials: P
authors.lastname: Lenartowicz
authors.affiliation: Faculty of Chemistry, Opole University, Oleska 48, 45-052 Opole, Poland.
authors.forename: Bartosz
authors.initials: B
authors.lastname: Oszywa
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland.
authors.forename: Michał
authors.initials: M
authors.lastname: Jewgiński
authors.affiliation: Faculty of Chemistry, Opole University, Oleska 48, 45-052 Opole, Poland.
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Pawełczak
authors.affiliation: Faculty of Chemistry, Opole University, Oleska 48, 45-052 Opole, Poland ; Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland.
authors.forename: Paweł
authors.initials: P
authors.lastname: Kafarski
keywords: Dehydropeptides; Enzyme inhibitors; Esterification; Molecular modeling