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Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.

Abstract：

:Retinoic acid receptor related orphan receptor γt (RORγt), has been identified as the master regulator of TH17-cell function and development, making it an attractive target for the treatment of autoimmune diseases by a small-molecule approach. Herein, we describe our investigations on a series of 4-aryl-thienyl acetamides, which were guided by insights from X-ray cocrystal structures. Efforts in targeting the cofactor-recruitment site from the 4-aryl group on the thiophene led to a series of potent binders with nanomolar activity in a primary human-TH17-cell assay. The observation of a DMSO molecule binding in a subpocket outside the LBD inspired the introduction of an acetamide into the benzylic position of these compounds. Hereby, a hydrogen-bond interaction of the introduced acetamide oxygen with the backbone amide of Glu379 was established. This greatly enhanced the cellular activity of previously weakly cell-active compounds. The best compounds combined potent inhibition of IL-17 release with favorable PK in rodents, with compound 32 representing a promising starting point for future investigations.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Narjes F,Xue Y,von Berg S,Malmberg J,Llinas A,Olsson RI,Jirholt J,Grindebacke H,Leffler A,Hossain N,Lepistö M,Thunberg L,Leek H,Aagaard A,McPheat J,Hansson EL,Bäck E,Tångefjord S,Chen R,Xiong Y,Hongbin G,Hansson

doi

10.1021/acs.jmedchem.8b00783

subject

Has Abstract

pub_date

2018-09-13 00:00:00

pages

7796-7813

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

61

pub_type

杂志文章

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