title: Novel hydroxamic acid-related phosphinates: inhibition of neutral aminopeptidase N (APN).
abstract: Here we describe the inhibitory activity toward neutral aminopeptidase of three new families of phosphinate inhibitors related in structure to hydroxamic acids. These compounds, even as racemic mixtures, are good inhibitors of APN and show strong structure activity relationship (SAR) depending on the substituents in P1 and P1' positions.
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland. mdrag@burnham.org
authors.forename: Marcin
authors.initials: M
authors.lastname: Drag
authors.forename: Renata
authors.initials: R
authors.lastname: Grzywa
authors.forename: Jozef
authors.initials: J
authors.lastname: Oleksyszyn
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D007700:Kinetics; D045726:Metalloproteases / Q000037:antagonists & inhibitors; D010721:Phosphinic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013237:Stereoisomerism
chemical_list: D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D010721:Phosphinic Acids; D011480:Protease Inhibitors; D045726:Metalloproteases; D018826:CD13 Antigens