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Novel triazolopyridylbenzamides as potent and selective p38α inhibitors

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
22
Issue
10
Identifiers
DOI: 10.1016/j.bmcl.2012.03.099
Keywords
  • P38α Inhibitors
  • Biaryl-Triazolopyridine Scaffold
  • Tnfα
  • Lps-Induced Endotoxemia
  • Rat Adjuvant-Induced Arthritis

Abstract

Abstract A new class of p38α inhibitors based on a biaryl-triazolopyridine scaffold was investigated. X-ray crystallographic data of the initial lead compound cocrystallised with p38α was crucial in order to uncover a unique binding mode of the inhibitor to the hinge region via a pair of water molecules. Synthesis and SAR was directed towards the improvement of binding affinity, as well as ADME properties for this new class of p38α inhibitors and ultimately afforded compounds showing good in vivo efficacy.

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