title: 2-Heteroaryl 2-substituted phenylketone derivatives and their inhibitory activity on platelet aggregation.
abstract: R 68070 and CV-4151 are two compounds possessing both thromboxane synthetase inhibitory activity and thromboxane receptor antagonist properties. 2-Heteroaryl 2-substituted phenylketone derivatives with a partial structural similarity to R 68070 and CV-4151, i.e. possessing a phenyl and a heteroaryl moiety, have been prepared and found to have antiplatelet activity. The compound 2-thienyl 2'-hydroxyphenyl ketone (4) was shown to completely inhibit platelet aggregation induced by arachidonic acid at a concentration of 5.0 microM. Structure-activity analysis indicated that the presence of a ketone group is an important requirement for this inhibitory activity. An o-hydroxyl substitution on the phenyl ring, and a 2-thienyl of heteroaryl ring might increase inhibitory activity.
authors.affiliation: School of Pharmacy, National Defense Medical Center, Taipei, Republic of China.
authors.forename: L Y
authors.initials: LY
authors.lastname: Hsu
authors.forename: C F
authors.initials: CF
authors.lastname: Lee
authors.forename: T C
authors.initials: TC
authors.lastname: Chou
authors.forename: Y A
authors.initials: YA
authors.lastname: Ding
mesh_terms: D000818:Animals; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry / Q000494:pharmacology*; D005343:Fibrinolytic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010421:Pentanoic Acids / Q000737:chemistry / Q000494:pharmacology*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship; D013929:Thromboxane B2 / Q000737:chemistry / Q000494:pharmacology; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*
chemical_list: D005229:Fatty Acids, Monounsaturated; D005343:Fibrinolytic Agents; D010421:Pentanoic Acids; D010975:Platelet Aggregation Inhibitors; D011725:Pyridines; D013929:Thromboxane B2; D013930:Thromboxane-A Synthase; C045446:isbogrel; C060219:ridogrel