title: Design, synthesis and in vitro activities on anti-platelet aggregation of 4-methoxybenzene-1,3-isophthalamides.
abstract: On the purpose of searching for the structure-activity relationship (SAR) and obtaining novel anti-platelet drugs, 41 4-methoxybenzene-1,3-isophthalamides have been described the synthesis process and in vitro activities on anti-platelet aggregation. The target compounds have been classified into four series: series 1 (ortho-substituted phenyl: 1a-1j), series 2 (meta-substituted phenyl: 2a-2k), series 3 (para-substituted phenyl: 3a-3l) and series 4 (aromatic of no substituted group and aromatic heterocyclic substituted groups: 4a-4h). The chemical structures of the target compounds were confirmed by MS, IR, (1)H NMR, and their in vitro activities on anti-platelet aggregation were tested and assessed by using Born test. The result showed that thirteen compounds 1c, 1d, 1i, 1j, 2g, 3a, 3c, 3d, 3f, 3h, 3l, 4b and 4c have superior anti-platelet aggregation activities than the reference drug Picotamide.
authors.affiliation: The College of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China. liuxiujie@hotmail.com
authors.forename: Xiu Jie
authors.initials: XJ
authors.lastname: Liu
authors.forename: Xin Xin
authors.initials: XX
authors.lastname: Shi
authors.forename: Yong Liang
authors.initials: YL
authors.lastname: Zhong
authors.forename: Ning
authors.initials: N
authors.lastname: Liu
authors.forename: Kai
authors.initials: K
authors.lastname: Liu
mesh_terms: D000818:Animals; D001792:Blood Platelets / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D015195:Drug Design; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D010795:Phthalic Acids / Q000737:chemistry / Q000494:pharmacology; D010797:Phthalimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
chemical_list: D010795:Phthalic Acids; D010797:Phthalimides; D010975:Platelet Aggregation Inhibitors; C011581:picotamide