title: Synthesis of N6-alkyl(aryl)-2-alkyl(aryl)thioadenosines as antiplatelet agents.
abstract: A series of novel N(6)-alkyl(aryl)-2-alkyl(aryl)thioadenosines were synthesized, and their human antiplatelet aggregation activities were evaluated by the stimulation of adenosine 5'-diphosphate (ADP). Some of these compounds showed strong activity, among which compound 5b(11) displayed the highest activity with an IC(50) value of 29 ± 3 μM. Furthermore, five compounds were tested against arachidonic acid (AA)-induced human platelet aggregation. The results showed that compound 5b(10) exhibited the highest activity with an IC(50) value of 3 ± 2 μM. The adenosine derivatives substituted with a phenethyl group at the N(6) position and a methylthio or ethylthio group at the C-2 position displayed high antiplatelet aggregation activity.
authors.affiliation: State Key Laboratory of Chemical Resource Engingeering, Department of Organic Chemistry, College of Science, Beijing University of Chemical Technology, Beijing 100029, China.
authors.forename: Guocheng
authors.initials: G
authors.lastname: Liu
authors.forename: Jiaxi
authors.initials: J
authors.lastname: Xu
authors.forename: Ning
authors.initials: N
authors.lastname: Chen
authors.forename: Si
authors.initials: S
authors.lastname: Zhang
authors.forename: Zhongren
authors.initials: Z
authors.lastname: Ding
authors.forename: Hongguang
authors.initials: H
authors.lastname: Du
mesh_terms: D000241:Adenosine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010975:Platelet Aggregation Inhibitors; D000241:Adenosine