141945-70-2Relevant academic research and scientific papers
Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1, adenosine receptor
Baraldi, Pier Giovanni,Romagnoli, Romeo,Pavani, Maria Giovanna,Del Carmen Nu?ez, Maria,Tabrizi, Mojgan Aghazadeh,Shryock, John C.,Leung, Edward,Moorman, Allan R.,Uluoglu, Canan,Iannotta, Valeria,Merighi, Stefania,Borea, Pier Andrea
, p. 794 - 809 (2007/10/03)
The current study describes the synthesis and biological evaluation of a novel series of 2-amino-3-naphthoylthiophenes, with variable modifications at the 4- and 5-position of the thiophene as well as the naphthoyl ring. Allosteric enhancer activity was m
Design and synthesis of novel CCR3 antagonists
Gong, Leyi,Hogg, J. Heather,Collier, James,Wilhelm, Robert S.,Soderberg, Carol
, p. 3597 - 3600 (2007/10/03)
As part of our investigation into the development of potent CCR3 antagonists, a series of piperidine analogues was designed and prepared. Exploration of the piperidine core examined both the basicity and the location of a nitrogen, as well as conformational variants. The bicyclo-piperidine 24c was found to be the most potent inhibitor of CCR3 with an IC50 of 0.0082 μM in the binding assay and 0.0024 μM in the chemotaxis assay.
