title: New azole antagonists with high affinity for the P2Y(1) receptor.
abstract: Five-membered-ring heterocyclic urea mimics have been found to be potent and selective antagonists of the P2Y1 receptor. SAR of the various heterocyclic replacements is presented, as well as side-chain SAR of the more potent thiadiazole ring system which leads to thiadiazole 4c as a new antiplatelet agent.
authors.affiliation: Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543, USA. rejean.ruel@umontreal.ca
authors.forename: Réjean
authors.initials: R
authors.lastname: Ruel
authors.forename: Alexandre
authors.initials: A
authors.lastname: L'Heureux
authors.forename: Carl
authors.initials: C
authors.lastname: Thibeault
authors.forename: Jean-Paul
authors.initials: JP
authors.lastname: Daris
authors.forename: Alain
authors.initials: A
authors.lastname: Martel
authors.forename: Laura A
authors.initials: LA
authors.lastname: Price
authors.forename: Qimin
authors.initials: Q
authors.lastname: Wu
authors.forename: Ji
authors.initials: J
authors.lastname: Hua
authors.forename: Ruth R
authors.initials: RR
authors.lastname: Wexler
authors.forename: Robert
authors.initials: R
authors.lastname: Rehfuss
authors.forename: Patrick Y S
authors.initials: PY
authors.lastname: Lam
mesh_terms: D040761:Biomimetic Materials / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D011485:Protein Binding; D058921:Purinergic P2Y Receptor Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D058472:Receptors, Purinergic P2Y1 / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry* / Q000494:pharmacology*; D014508:Urea / Q000737:chemistry
chemical_list: D058921:Purinergic P2Y Receptor Antagonists; D058472:Receptors, Purinergic P2Y1; D013830:Thiadiazoles; D014508:Urea