Antiallergic Activity Profile in Vitro RBL-2H3 and in Vivo Passive Cutaneous Anaphylaxis Mouse Model of New Si la-Substituted 1,3,4-Oxadiazoles

作者：Reddy Guda Dinneswara; Park Sae Jin; Cho Hyeon Mo; Kim Tack Joong^*; Lee Myong Euy

来源：Journal of Medicinal Chemistry, 2012, 55(14): 6438-6444.

DOI：10.1021/jm300421h

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-alpha 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.

• 出版日期2012-7-26