Document Report Card
Basic Information
ID: ALA3399948
Journal: Bioorg Med Chem Lett
Title: Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
Authors: Esteve C, González J, Gual S, Vidal L, Alzina S, Sentellas S, Jover I, Horrillo R, De Alba J, Miralpeix M, Tarrasón G, Vidal B.
Abstract: Synthesis and SAR of a series of 7-azaindoles as Orai channel inhibitors showing good potency inhibiting IL-2 production in Jurkat cells is described. Compound 14d displaying best pharmacokinetic properties was further characterized in a model of allergen induced asthma showing inhibition in the number of eosinophils in BALF. High lipophilicity remains as one of the main challenges for this class of compounds.
CiteXplore: 25690784