title: Synthesis of heparin-like antithrombotics having perphosphorylated thrombin binding domains.
abstract: The synthesis of three heparin analogues (i.e. compounds VI-VIII) having perphosphorylated thrombin binding domains (TBDs) is reported. These compounds were tested in vitro for their antithrombin III (ATIII)-mediated anti-Xa and antithrombin activities. Conjugates VI and VIII show a remarkable increase in antithrombin activity compared to the structurally related conjugates with persulfated TBDs (i.e. compounds IV and V), whereas compound VII displays a diminished activity.
authors.affiliation: Leiden Institute of Chemistry, Gorlaeus Laboratories, The Netherlands.
authors.forename: R C
authors.initials: RC
authors.lastname: Buijsman
authors.forename: J E
authors.initials: JE
authors.lastname: Basten
authors.forename: C M
authors.initials: CM
authors.lastname: Dreef-Tromp
authors.forename: G A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: C A
authors.initials: CA
authors.lastname: van Boeckel
authors.forename: J H
authors.initials: JH
authors.lastname: van Boom
mesh_terms: D000991:Antithrombins / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D002236:Carbohydrate Conformation; D002240:Carbohydrate Sequence; D006493:Heparin / Q000031:analogs & derivatives*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008969:Molecular Sequence Data; D010766:Phosphorylation; D013917:Thrombin / Q000378:metabolism*
chemical_list: D000991:Antithrombins; D006493:Heparin; D013917:Thrombin