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Journal of Medicinal Chemistry 2019-Mar

Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold.

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Masayuki Kotoku
Takaki Maeba
Shingo Fujioka
Masahiro Yokota
Noriyoshi Seki
Keisuke Ito
Yoshihiro Suwa
Taku Ikenogami
Kazuyuki Hirata
Yasunori Hase

Keywords

Abstract

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.

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