Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

JJ, Duan; Z, Lu; B, Jiang; S, Stachura; CA, Weigelt; JS, Sack; J, Khan; M, Ruzanov; MA, Galella; DR, Wu; M, Yarde; DR, Shen; DJ, Shuster; V, Borowski; JH, Xie; L, Zhang; S, Vanteru; AK, Gupta; A, Mathur; Q, Zhao; W, Foster; LM, Salter-Cid; PH, Carter; TGM, Dhar

doi:10.1021/acsmedchemlett.9b00010

Public

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Shared by NobleBlocks on Feb 26, 2019 • 12:00 AM UTC

Authors:

Duan JJ

Lu Z

Jiang B

Abstract

A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide <b>1</b>. Through a combination of structure-based design and structure-activity relationship studies, a polar set of amides at...

Research Assistant

AI chat, annotations, notes & similar papers

Finding related papers...

Discussions

(0)

No comments yet

Be the first to share your thoughts!