title: [Design, synthesis of novel N, N'-bis-(halogenophenyl)-4- methoxybenzene-1, 3-disulfonamides and evaluation of their anti-platelet aggregation activity].
abstract: Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.
authors.forename: Gui-Ang
authors.initials: GA
authors.lastname: Li
authors.forename: Xiao
authors.initials: X
authors.lastname: Wang
authors.forename: Xia
authors.initials: X
authors.lastname: Meng
authors.forename: Yong-Bin
authors.initials: YB
authors.lastname: Lin
authors.forename: Xu
authors.initials: X
authors.lastname: Li
authors.forename: Xiu-Jie
authors.initials: XJ
authors.lastname: Liu
mesh_terms: D000244:Adenosine Diphosphate; D015195:Drug Design; D010795:Phthalic Acids; D010974:Platelet Aggregation; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D010795:Phthalic Acids; D010975:Platelet Aggregation Inhibitors; D013449:Sulfonamides; D000244:Adenosine Diphosphate; C011581:picotamide