Details

Autor(en) / Beteiligte

• Schulte, Christie A.
• Deaton, David N.
• Diaz, Elsie
• Do, Young
• Gampe, Robert T.
• Guss, Jeffrey H.
• Hancock, Ashley P.
• Hobbs, Heather
• Hodgson, Simon T.
• Holt, Jason
• Jeune, Michael R.
• Kahler, Kirsten M.
• Kramer, H. Fritz
• Le, Joelle
• Mortenson, Paul N.
• Musetti, Caterina
• Nolte, Robert T.
• Orband-Miller, Lisa A.
• Peckham, Gregory E.
• Petrov, Kim G.
• Pietrak, Beth L.
• Poole, Chuck
• Price, Daniel J.
• Saxty, Gordon
• Shillings, Anthony
• Smalley, Terrence L.
• Somers, Don O.
• Stewart, Eugene L.
• Stuart, J. Darren
• Thomson, Stephen A.

Titel

A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128113-128113, Article 128113

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2021

Quelle

MEDLINE

Beschreibungen/Notizen

• Through an internal virtual screen performed at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imidazopyridine inhibitor of H-PGDS, 20b. Herein, describes the identification of 2 classes of inhibitors, their syntheses, and their challenges. [Display omitted] Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imidazopyridine inhibitor of H-PGDS, 20b. Herein, describes the identification of 2 classes of inhibitors, their syntheses, and their challenges.