4-aminopiperidine and Obesity

4-aminopiperidine has been researched along with Obesity* in 1 studies

Other Studies

1 other study(ies) available for 4-aminopiperidine and Obesity

Article	Year
Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity. Bioorganic & medicinal chemistry letters, 2006, Oct-15, Volume: 16, Issue:20 A substituted 4-aminopiperidine was identified as showing activity in an MCH assay from an HTS effort. Subsequent structural modification of the scaffold led to the identification of a number of active MCH antagonists. 3,5-Dimethoxy-N-(1-(naphthalen-2-ylmethyl)piperidin-4-yl)benzamide (5c) was among those with the highest binding affinity to the MCH receptor (K(i)=27nM), when variations were made at benzoyl and naphthylmethyl substitution sites from the initial HTS hit. Further optimization via piperidine ring contraction resulted in enhanced MCH activity in a 3-aminopyrrolidine series, where (R)-3,5-dimethoxy-N-(1-(naphthalen-2-ylmethyl)-pyrrolidin-3-yl)benzamide (10i) was found to be an excellent MCH antagonist (K(i)=7nM). Topics: Binding, Competitive; Drug Evaluation, Preclinical; Humans; Molecular Structure; Obesity; Piperidines; Pyrrolidines; Receptors, Somatostatin; Stereoisomerism; Structure-Activity Relationship	2006

Article

Year

Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity.

Bioorganic & medicinal chemistry letters, 2006, Oct-15, Volume: 16, Issue:20

A substituted 4-aminopiperidine was identified as showing activity in an MCH assay from an HTS effort. Subsequent structural modification of the scaffold led to the identification of a number of active MCH antagonists. 3,5-Dimethoxy-N-(1-(naphthalen-2-ylmethyl)piperidin-4-yl)benzamide (5c) was among those with the highest binding affinity to the MCH receptor (K(i)=27nM), when variations were made at benzoyl and naphthylmethyl substitution sites from the initial HTS hit. Further optimization via piperidine ring contraction resulted in enhanced MCH activity in a 3-aminopyrrolidine series, where (R)-3,5-dimethoxy-N-(1-(naphthalen-2-ylmethyl)-pyrrolidin-3-yl)benzamide (10i) was found to be an excellent MCH antagonist (K(i)=7nM).

Topics: Binding, Competitive; Drug Evaluation, Preclinical; Humans; Molecular Structure; Obesity; Piperidines; Pyrrolidines; Receptors, Somatostatin; Stereoisomerism; Structure-Activity Relationship

2006