title: A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor.
abstract: A novel series of P2Y(12) antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds showed P2Y(12) antagonistic activities in the sub-micromolar range.
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca R&D, Pepparedsleden 1, S-43183 Mölndal, Sweden. Peter.Bach@astrazeneca.com
authors.forename: Peter
authors.initials: P
authors.lastname: Bach
authors.forename: Jonas
authors.initials: J
authors.lastname: Boström
authors.forename: Kay
authors.initials: K
authors.lastname: Brickmann
authors.forename: J J J
authors.initials: JJ
authors.lastname: van Giezen
authors.forename: Ragnar
authors.initials: R
authors.lastname: Hovland
authors.forename: Annika U
authors.initials: AU
authors.lastname: Petersson
authors.forename: Asim
authors.initials: A
authors.lastname: Ray
authors.forename: Fredrik
authors.initials: F
authors.lastname: Zetterberg
mesh_terms: D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D058914:Purinergic Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry*; D058925:Receptors, Purinergic P2Y12 / Q000378:metabolism; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D010879:Piperazines; D010975:Platelet Aggregation Inhibitors; D058914:Purinergic Antagonists; D011725:Pyridines; D058925:Receptors, Purinergic P2Y12; D014508:Urea