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Bioorg Med Chem Lett. 2015 Mar 15;25(6):1217-22. doi: 10.1016/j.bmcl.2015.01.063. Epub 2015 Feb 4.

Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.

Author information

1
Almirall Research Center, Almirall, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain.
2
Almirall Research Center, Almirall, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain. Electronic address: bernat.vidal@almirall.com.

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.

KEYWORDS:

CRAC channel; IL-2 inhibitors; LAD2; OVA model; Orai inhibitors

PMID:
25690784
DOI:
10.1016/j.bmcl.2015.01.063
[Indexed for MEDLINE]

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