208646-35-9Relevant academic research and scientific papers
A highly efficient and selective AuI-catalyzed tandem synthesis of diversely substituted pyrrolo[1,2-a]quinolines in aqueous media
Liu, Xin-Yuan,Che, Chi-Ming
, p. 3805 - 3810 (2008/12/23)
(Chemical Equation Presented) Bicycles built in water: The Au I-catalyzed tandem cyclization of 1-amino-4-alkynes with alkynes in water offers a simple and efficient method for the synthesis of diversely substituted pyrrolo[1,2-a]quinolines with good to excellent product yields and excellent regio- and chemoselectivities (see scheme).
7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase
Duplantier, Allen J.,Andresen, Catharine J.,Cheng, John B.,Cohan, Victoria L.,Decker, Christian,DiCapua, Frank M.,Kraus, Kenneth G.,Johnson, Kerry L.,Turner, Claudia R.,UmLand, John P.,Watson, John W.,Wester, Ronald T.,Williams, Alison S.,Williams, John A.
, p. 2268 - 2277 (2007/10/03)
High-throughput file screening against inhibition of human lung PDE4 led to the discovery of 3-ethyl-1-(4-fluorophenyl)-6-phenyl-7-oxo-4,5,6,7,- tetrahydro-1H-pyrazolo[3,4-c]pyridine (11) as a novel PDE4 inhibitor. Subsequent SAR development, using an eosinophil PDE assay, led to analogues up to 50-fold more potent than 11 with IC50 values of 0.03-1.6 μM. One such compound, CP-220,629 (22) (IC50 = 0.44 μM), was efficacious in the guinea pig aerosolized antigen induced airway obstruction assay (ED50 2.0 mg/kg, po) and demonstrated a significant reduction in eosinophil (55%), neutrophil (65%), and IL-1β (82%) responses to antigen challenge in atopic monkeys (10 mg/kg, po).
