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Acta Pharmaceutica Sinica ; (12): 917-925, 2008.
Artigo em Chinês | WPRIM | ID: wpr-232668

RESUMO

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.


Assuntos
Animais , Camundongos , Ratos , Anti-Inflamatórios , Química , Farmacologia , Usos Terapêuticos , Artrite Reumatoide , Tratamento Farmacológico , Glucuronidase , Metabolismo , Cetonas , Química , Farmacologia , Usos Terapêuticos , Macrófagos Peritoneais , Metabolismo , Neutrófilos , Glicoproteínas da Membrana de Plaquetas , Receptores Acoplados a Proteínas G , Relação Estrutura-Atividade , Fator de Necrose Tumoral alfa
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