Pyrazolopyridines as potent PDE4B inhibitors: 5-Heterocycle SAR

…, JN Hamblin, S Holman, MR Johnson, PS Jones…

Index: Mitchell, Charlotte J.; Ballantine, Stuart P.; Coe, Diane M.; Cook, Caroline M.; Delves, Christopher J.; Dowle, Mike D.; Edlin, Chris D.; Hamblin, J. Nicole; Holman, Stuart; Johnson, Martin R.; Jones, Paul S.; Keeling, Sue E.; Kranz, Michael; Lindvall, Mika; Lucas, Fiona S.; Neu, Margarete; Solanke, Yemisi E.; Somers, Don O.; Trivedi, Naimisha A.; Wiseman, Joanne O. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5803 - 5806

Full Text: HTML

Citation Number: 21

Abstract

Following the discovery of 4-(substituted amino)-1-alkyl-pyrazolo [3, 4-b] pyridine-5- carboxamides as potent and selective phosphodiesterase 4B inhibitors,[Hamblin, JN; Angell, T.; Ballentine, S., et al. Bioorg. Med. Chem. Lett. 2008, 18, 4237] the SAR of the 5- position was investigated further. A range of substituted heterocycles showed good potencies against PDE4. Optimisation using X-ray crystallography and computational ...