1622208-41-6Relevant articles and documents
Synthesis and SAR Studies of 1 H-Pyrrolo[2,3- b]pyridine-2-carboxamides as Phosphodiesterase 4B (PDE4B) Inhibitors
Vadukoot, Anish K.,Sharma, Swagat,Aretz, Christopher D.,Kumar, Sushil,Gautam, Nagsen,Alnouti, Yazen,Aldrich, Amy L.,Heim, Cortney E.,Kielian, Tammy,Hopkins, Corey R.
, p. 1848 - 1854 (2020)
Herein we report the synthesis, SAR, and biological evaluation of a series of 1H-pyrrolo[2,3-b]pyridine-2-carboxamide derivatives as selective and potent PDE4B inhibitors. Compound 11h is a PDE4B preferring inhibitor and exhibited acceptable in vitro ADME and significantly inhibited TNF-α release from macrophages exposed to pro-inflammatory stimuli (i.e., lipopolysaccharide and the synthetic bacterial lipopeptide Pam3Cys). In addition, 11h was selective against a panel of CNS receptors and represents an excellent lead for further optimization and preclinical testing in the setting of CNS diseases.