Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold
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https://figshare.com/articles/dataset/Discovery_of_Second_Generation_ROR_Inhibitors_Composed_of_an_Azole_Scaffold/7792466
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资源简介：
Starting from a previously reported
RORγ inhibitor (1), successive efforts to improve
in vivo potency were continued.
Introduction of metabolically beneficial motifs in conjunction with
scaffold hopping was examined, resulting in discovery of the second
generation RORγ inhibitor composed of a 4-(isoxazol-3-yl)butanoic
acid scaffold (24). Compound 24 achieved
a 10-fold improvement in in vivo potency in a mouse CD3 challenge
model along with significant anti-inflammatory effects in a mouse
dermatitis model.
创建时间：
2019-03-01
