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.
Publication types
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English Abstract
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Anti-Inflammatory Agents / therapeutic use
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Arthritis, Rheumatoid / drug therapy
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Glucuronidase / metabolism
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Ketones / chemical synthesis*
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Ketones / chemistry
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Ketones / pharmacology*
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Ketones / therapeutic use
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Macrophages, Peritoneal / metabolism
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Mice
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Neutrophils / enzymology
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Platelet Membrane Glycoproteins / antagonists & inhibitors*
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Rats
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Receptors, G-Protein-Coupled / antagonists & inhibitors*
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Structure-Activity Relationship
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Anti-Inflammatory Agents
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Ketones
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Platelet Membrane Glycoproteins
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Receptors, G-Protein-Coupled
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Tumor Necrosis Factor-alpha
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platelet activating factor receptor
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Glucuronidase