161291-74-3Relevant academic research and scientific papers
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
Buettelmann, Bernd,Peters, Jens-Uwe,Ceccarelli, Simona,Kolczewski, Sabine,Vieira, Eric,Prinssen, Eric P.,Spooren, Will,Schuler, Franz,Huwyler, Joerg,Porter, Richard H. P.,Jaeschke, Georg
, p. 1892 - 1897 (2006)
Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.
Diarylsulfonamides as selective, non-peptidic thrombin inhibitors
Weber, Ingo R.,Neidlein, Richard,Von Der Saal, Wolfgang,Grams, Frank,Leinert, Herbert,Strein, Klaus,Engh, Richard A.,Kucznierz, Ralf
, p. 1613 - 1618 (2007/10/03)
Based on the structures of aminopyridine thrombin inhibitors (1), a series of aminoalkyl- and guanidinoalkyl-substituted diarylsulfonamides were prepared. The most potent derivative, N-[3-(4-guanidinobutoxy)-5-methyl- phenyl]-benzenesulfonamide (6c) had Ki = 0.18 μM for thrombin and did not inhibit trypsin, plasmin, or factor Xa. Comparison of the X-ray structures of the thrombin / 1b and the thrombin / 6e complexes revealed important aspects which govern the binding of such diarylsulfonamides to thrombin.
