title: Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides.
abstract: In our search for new compounds among the structural analogues of the Picotamide acting on antiplatelet aggregation activities, a new series 2 of 4-ethoxyisophthal-amides were synthesized and their in vitro anti-platelet aggregation activities were evaluated by Born's test in comparison with their structural analogues of the series 1 of 4-methoxyisophthal-amides. The results revealed, among the series 2, six compounds 200, 2a, 2k, 2n, 2q and 2r displayed good antiplatelet aggregation activities in vitro induced by 5.0 mM ADP with IC50 values ranging over 0.35 μM - 0.77 μM. And of which, compound 2a exhibited the highest in vitro activity superior than two control drugs Picotamide and Aspirin. From a structure-affnity-'Relationship (SAR) pointed of some insight in the view of the role played by 4-ethoxy derivatives.
authors.affiliation: College of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China. liuxiujie@hotmail.com.
authors.forename: Xiu J
authors.initials: XJ
authors.lastname: Liu
authors.forename: Tian En
authors.initials: TE
authors.lastname: Shi
authors.forename: Xiao
authors.initials: X
authors.lastname: Wang
authors.forename: Ting T
authors.initials: TT
authors.lastname: Wei
authors.forename: Xia
authors.initials: X
authors.lastname: Meng
mesh_terms: D001241:Aspirin / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D010795:Phthalic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship; D013329:Structure-Activity Relationship
chemical_list: D010795:Phthalic Acids; D010975:Platelet Aggregation Inhibitors; C011581:picotamide; D001241:Aspirin