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J Med Chem. 2012 Jul 26;55(14):6438-44. doi: 10.1021/jm300421h. Epub 2012 Jul 17.

Antiallergic activity profile in vitro RBL-2H3 and in vivo passive cutaneous anaphylaxis mouse model of new sila-substituted 1,3,4-oxadiazoles.

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Department of Chemistry and Medical Chemistry, College of Science and Technology, Research and Education Center for Advanced Silicon Materials, Yonsei University, Wonju, Gangwon-do 220-710, South Korea.

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  • J Med Chem. 2012 Aug 23;55(16):7296.


A new class of sila-substituted 1,3,4-oxadiazoles was synthesized and evaluated for antiallergic activity using RBL-2H3 as the in vitro model and the in vivo anaphylactic mouse model. We observed that compound 5c effectively suppressed DNP-HSA-induced mast cell degranulation, compared to carbon analogue 9, and also suppressed the expression of TNF-α mRNA and Akt phosphorylation in antigen-stimulated RBL-2H3 cells. We also studied the effect of 5c in an in vivo passive cutaneous anaphylaxis (PCA) mouse model. The suppression by 5c was more effective than that by diphenylhydramine (DPH), a typical anti-histamine drug.

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