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Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents. 2012

Hao Zhang, and Jun Liu, and Luyong Zhang, and Lingyi Kong, and Hequan Yao, and Hongbin Sun
Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, Nanjing, China.

Ticagrelor (1) is the first reversible P2Y12 receptor antagonist blocking adenine diphosphate (ADP)-induced platelet aggregation with rapid onset and offset of effects. In this study, synthesis of ticagrelor and its derivatives has been accomplished in a convergent way. The compound design was based on modifications of ticagrelor and its major metabolite (33) in order to ameliorate their pharmacokinetic properties and dosing profile. The final compounds (1a-g, 35a-g) were evaluated for their inhibitory effect on ADP-induced platelet aggregation in rats. The assay results showed that some compounds (e.g., 1b, 1d, 33, 35b, 35f) exhibited comparable potency with that of ticagrelor.

UI MeSH Term Description Entries
D010975 Platelet Aggregation Inhibitors Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. Antiaggregants, Platelet,Antiplatelet Agent,Antiplatelet Agents,Antiplatelet Drug,Blood Platelet Aggregation Inhibitor,Blood Platelet Antagonist,Blood Platelet Antiaggregant,PAR-1 Antagonists,Platelet Aggregation Inhibitor,Platelet Antagonist,Platelet Antagonists,Platelet Antiaggregant,Platelet Antiaggregants,Platelet Inhibitor,Protease-Activated Receptor-1 Antagonists,Antiplatelet Drugs,Blood Platelet Aggregation Inhibitors,Blood Platelet Antagonists,Blood Platelet Antiaggregants,Platelet Inhibitors,Agent, Antiplatelet,Aggregation Inhibitor, Platelet,Antagonist, Blood Platelet,Antagonist, Platelet,Antiaggregant, Blood Platelet,Antiaggregant, Platelet,Drug, Antiplatelet,Inhibitor, Platelet,Inhibitor, Platelet Aggregation,PAR 1 Antagonists,Platelet Antagonist, Blood,Platelet Antiaggregant, Blood,Protease Activated Receptor 1 Antagonists
D001792 Blood Platelets Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation. Platelets,Thrombocytes,Blood Platelet,Platelet,Platelet, Blood,Platelets, Blood,Thrombocyte
D000077486 Ticagrelor An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION. 3-(7-((2-(3,4-Difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-(1-3)-triazolo(4,5-d)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol,AZD 6140,AZD-6140,AZD6140,Brilinta,Brilique
D000241 Adenosine A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter. Adenocard,Adenoscan
D000244 Adenosine Diphosphate Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position. ADP,Adenosine Pyrophosphate,Magnesium ADP,MgADP,Adenosine 5'-Pyrophosphate,5'-Pyrophosphate, Adenosine,ADP, Magnesium,Adenosine 5' Pyrophosphate,Diphosphate, Adenosine,Pyrophosphate, Adenosine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D058921 Purinergic P2Y Receptor Antagonists Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes. ADP Receptor Antagonist,ADP Receptor Blocker,Adenosine Diphosphate Receptor Antagonist,P2Y Purinoceptor Antagonist,P2Y1 Purinoceptor Antagonist,P2Y12 Purinoceptor Antagonist,P2Y12 Receptor Antagonist,P2Y2 Purinoceptor Antagonist,Purinergic P2Y Receptor Antagonist,Purinergic P2Y1 Receptor Antagonist,Purinergic P2Y12 Receptor Antagonist,Purinergic P2Y2 Receptor Antagonist,ADP Receptor Antagonists,ADP Receptor Blockers,Adenosine Diphosphate Receptor Antagonists,P2Y Purinoceptor Antagonists,P2Y1 Purinoceptor Antagonists,P2Y12 Purinoceptor Antagonists,P2Y12 Receptor Antagonists,P2Y2 Purinoceptor Antagonists,Purinergic P2Y1 Receptor Antagonists,Purinergic P2Y12 Receptor Antagonists,Purinergic P2Y2 Receptor Antagonists,Antagonist, ADP Receptor,Antagonist, P2Y Purinoceptor,Antagonist, P2Y1 Purinoceptor,Antagonist, P2Y12 Purinoceptor,Antagonist, P2Y12 Receptor,Antagonist, P2Y2 Purinoceptor,Antagonists, ADP Receptor,Antagonists, P2Y Purinoceptor,Antagonists, P2Y1 Purinoceptor,Antagonists, P2Y12 Purinoceptor,Antagonists, P2Y12 Receptor,Antagonists, P2Y2 Purinoceptor,Blocker, ADP Receptor,Purinoceptor Antagonist, P2Y,Purinoceptor Antagonist, P2Y1,Purinoceptor Antagonist, P2Y12,Purinoceptor Antagonist, P2Y2,Purinoceptor Antagonists, P2Y,Purinoceptor Antagonists, P2Y1,Purinoceptor Antagonists, P2Y12,Purinoceptor Antagonists, P2Y2,Receptor Antagonist, ADP,Receptor Antagonist, P2Y12,Receptor Antagonists, ADP,Receptor Antagonists, P2Y12,Receptor Blocker, ADP,Receptor Blockers, ADP
D058925 Receptors, Purinergic P2Y12 A subclass of purinergic P2Y receptors that have a preference for ADP binding and are coupled to GTP-BINDING PROTEIN ALPHA SUBUNIT, GI. The P2Y12 purinergic receptors are found in PLATELETS where they play an important role regulating PLATELET ACTIVATION. P2T Purinoceptor,P2Y(ADP) Receptor,P2Y(T) Receptor,P2Y12 Purinoceptor,P2Y12 Purinoceptors,Purinergic Receptor P2Y, G-Protein Coupled, 12,Purinergic Receptor P2Y12,Purinoceptor P2T,Purinoceptor P2Y12,P2T, Purinoceptor,P2Y12 Receptors, Purinergic,P2Y12, Purinergic Receptor,P2Y12, Purinoceptor,Purinergic P2Y12 Receptors,Purinoceptor, P2T,Purinoceptor, P2Y12,Purinoceptors, P2Y12

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