piperidines and pyrazolone

piperidines has been researched along with pyrazolone* in 1 studies

Other Studies

1 other study(ies) available for piperidines and pyrazolone

Article	Year
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists. Bioorganic & medicinal chemistry letters, 2006, Volume: 16, Issue:3 A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity. Topics: Analgesics; Animals; Binding Sites; Bridged Bicyclo Compounds, Heterocyclic; Feeding Behavior; Models, Biological; Piperidines; Pyrazoles; Pyrazolones; Pyrimidinones; Receptor, Cannabinoid, CB1; Rimonabant; Rodentia; Structure-Activity Relationship	2006

Article

Year

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.

Bioorganic & medicinal chemistry letters, 2006, Volume: 16, Issue:3

A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.

Topics: Analgesics; Animals; Binding Sites; Bridged Bicyclo Compounds, Heterocyclic; Feeding Behavior; Models, Biological; Piperidines; Pyrazoles; Pyrazolones; Pyrimidinones; Receptor, Cannabinoid, CB1; Rimonabant; Rodentia; Structure-Activity Relationship

2006