7JR6

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

Schulte, C.A., Deaton, D.N., Diaz, E., Do, Y., Gampe, R.T., Guss, J.H., Hancock, A.P., Hobbs, H., Hodgson, S.T., Holt, J., Jeune, M.R., Kahler, K.M., Kramer, H.F., Le, J., Mortenson, P.N., Musetti, C., Nolte, R.T., Orband-Miller, L.A., Peckham, G.E., Petrov, K.G., Pietrak, B.L., Poole, C., Price, D.J., Saxty, G., Shillings, A., Smalley Jr., T.L., Somers, D.O., Stewart, E.L., Stuart, J.D., Thomson, S.A.

(2021) Bioorg Med Chem Lett 47: 128113-128113

• PubMed: 33991628 Search on PubMed
• DOI: https://doi.org/10.1016/j.bmcl.2021.128113
• Primary Citation of Related Structures:  
  6ZTC, 7JR6, 7JR8


• PubMed Abstract: 
  

  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.

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Organizational Affiliation: 

GlaxoSmithKline, 5 Moore Drive, P.O. Box 13398, Research Triangle Park, NC 27709, United States. Electronic address: [email protected].