[Synthesis and antiinflammation activity of aromatic aminoketone compounds, a new type of PAF-receptor antagonist].
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.
Mou
Li-yuan
LY
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Lin
Zi-yun
ZY
Liu
Jie
J
Zhang
Qi-dong
QD
Zhu
Li-ya
LY
Wang
Wen-jie
WJ
Nie
Zhen-gui
ZG
He
Yu
Y
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
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