720704-63-2Relevant academic research and scientific papers
Pyrazolopyridines as potent PDE4B inhibitors: 5-Heterocycle SAR
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.
, p. 5803 - 5806 (2010)
Following the discovery of 4-(substituted amino)-1-alkyl-pyrazolo[3,4-b] pyridine-5-carboxamides as potent and selective phosphodiesterase 4B inhibitors, [Hamblin, J. N.; 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 modelling led to the discovery of 16, with sub-nM inhibition of LPS-induced TNF-α production from isolated human peripheral blood mononuclear cells.
