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Eur J Med Chem ; 60: 365-75, 2013 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-23314050

RESUMEN

α-Santonin derived new series of 1,2,3-triazoles synthesized through Azide-Alkyne Huisgen 1,3-dipolar cycloaddition reaction between substituted aryl azide and a propargylated α-desmotrosantonin were bio-evaluated for their diminutive effect on ConA induced T-cell and LPS induced B-cell proliferation. Interestingly, most of the synthesized compounds showed better immunosuppressant activity than α-santonin. Triazole derivatives 9, 10, 17, 18, 29, and 30 displayed significant diminutive effect on cell proliferation. Compounds 12 and 13 were found selective against ConA T-cell proliferation exhibiting >90% inhibition at 1 × 10(-6) M concentration. The present study resulted in identification of several triazole derivatives as effective immunosuppressive agents.


Asunto(s)
Santonina/química , Triazoles/farmacología , Animales , Linfocitos B/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Concanavalina A/farmacología , Lipopolisacáridos/farmacología , Ratones , Ratones Endogámicos BALB C , Estructura Molecular , Relación Estructura-Actividad , Linfocitos T/efectos de los fármacos , Triazoles/síntesis química , Triazoles/química
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