title: [Synthesis and antiinflammation activity of aromatic aminoketone compounds, a new type of PAF-receptor antagonist].
abstract: A series of aromatic aminoketones were synthesized by Mannich reaction. Structures of these compounds were confirmed by 1H NMR, MS and HRMS or element analysis. Pharmacological screening showed that most target compounds inhibited the release of beta-glucuronidase in polymorphonuclear leucocytes by PAF (platelet activating factor) and compounds MA12, MA13, MA18, MA21 and MA33 were more active. The study suggests that target compounds are potential PAF receptor antagonists and their anti-inflammatory activities are due to the inhibition of release of lysosomal enzyme.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors.forename: Li-yuan
authors.initials: LY
authors.lastname: Mou
authors.forename: Zi-yun
authors.initials: ZY
authors.lastname: Lin
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.forename: Qi-dong
authors.initials: QD
authors.lastname: Zhang
authors.forename: Li-ya
authors.initials: LY
authors.lastname: Zhu
authors.forename: Wen-jie
authors.initials: WJ
authors.lastname: Wang
authors.forename: Zhen-gui
authors.initials: ZG
authors.lastname: Nie
authors.forename: Yu
authors.initials: Y
authors.lastname: He
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D005966:Glucuronidase / Q000378:metabolism; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017737:Macrophages, Peritoneal / Q000378:metabolism; D051379:Mice; D009504:Neutrophils / Q000201:enzymology; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
chemical_list: D000893:Anti-Inflammatory Agents; D007659:Ketones; D010980:Platelet Membrane Glycoproteins; D043562:Receptors, G-Protein-Coupled; D014409:Tumor Necrosis Factor-alpha; C039351:platelet activating factor receptor; D005966:Glucuronidase