azd3988 and Obesity

azd3988 has been researched along with Obesity* in 1 studies

Other Studies

1 other study(ies) available for azd3988 and Obesity

Article	Year
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorganic & medicinal chemistry letters, 2012, Jun-15, Volume: 22, Issue:12 A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clinical candidate 53 (AZD3988), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clinical in vivo efficacy that could be rationalised through a PK/PD relationship. Topics: Animals; Diabetes Mellitus; Diacylglycerol O-Acyltransferase; Dogs; Drug Design; Drug Evaluation, Preclinical; Enzyme Inhibitors; Half-Life; High-Throughput Screening Assays; Humans; Hypoglycemic Agents; Ligands; Mice; Obesity; Oxadiazoles; Quantitative Structure-Activity Relationship; Rats	2012

Article

Year

Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.

Bioorganic & medicinal chemistry letters, 2012, Jun-15, Volume: 22, Issue:12

A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clinical candidate 53 (AZD3988), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clinical in vivo efficacy that could be rationalised through a PK/PD relationship.

Topics: Animals; Diabetes Mellitus; Diacylglycerol O-Acyltransferase; Dogs; Drug Design; Drug Evaluation, Preclinical; Enzyme Inhibitors; Half-Life; High-Throughput Screening Assays; Humans; Hypoglycemic Agents; Ligands; Mice; Obesity; Oxadiazoles; Quantitative Structure-Activity Relationship; Rats

2012