A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Christie A Schulte, David N Deaton, Elsie Diaz, Young Do, Robert T Gampe, Jeffrey H Guss, Ashley P Hancock, Heather Hobbs, Simon T Hodgson, Jason Holt, Michael R Jeune, Kirsten M Kahler, H Fritz Kramer, Joelle Le, Paul N Mortenson, Caterina Musetti, Robert T Nolte, Lisa A Orband-Miller, Gregory E Peckham, Kim G Petrov, Beth L Pietrak, Chuck Poole, Daniel J Price, Gordon Saxty, Anthony Shillings, Terrence L Smalley, Don O Somers, Eugene L Stewart, J Darren Stuart, Stephen A Thomson
Bioorganic & medicinal chemistry letters 2021 Sep 01Through 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. Copyright © 2021 Elsevier Ltd. All rights reserved.
Citation
Christie A Schulte, David N Deaton, Elsie Diaz, Young Do, Robert T Gampe, Jeffrey H Guss, Ashley P Hancock, Heather Hobbs, Simon T Hodgson, Jason Holt, Michael R Jeune, Kirsten M Kahler, H Fritz Kramer, Joelle Le, Paul N Mortenson, Caterina Musetti, Robert T Nolte, Lisa A Orband-Miller, Gregory E Peckham, Kim G Petrov, Beth L Pietrak, Chuck Poole, Daniel J Price, Gordon Saxty, Anthony Shillings, Terrence L Smalley, Don O Somers, Eugene L Stewart, J Darren Stuart, Stephen A Thomson. A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors. Bioorganic & medicinal chemistry letters. 2021 Sep 01;47:128113
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PMID: 33991628
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