bi-78d3 and 5-(5-nitrothiazol-2-ylthio)-1-3-4-thiadiazol-2-amine

bi-78d3 has been researched along with 5-(5-nitrothiazol-2-ylthio)-1-3-4-thiadiazol-2-amine* in 1 studies

Other Studies

1 other study(ies) available for bi-78d3 and 5-(5-nitrothiazol-2-ylthio)-1-3-4-thiadiazol-2-amine

Article	Year
Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase. Journal of medicinal chemistry, 2009, Apr-09, Volume: 52, Issue:7 We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. The compounds are substrate competitive inhibitors that bind to the docking site of the kinase. The reported medicinal chemistry and structure-based optimizations studies resulted in the discovery of selective and potent thiadiazole JNK inhibitors that display promising in vivo activity in mouse models of insulin insensitivity. Topics: Activating Transcription Factor 2; Animals; Binding Sites; Diabetes Mellitus, Type 2; Drug Design; HeLa Cells; Humans; Hypoglycemic Agents; Insulin Resistance; JNK Mitogen-Activated Protein Kinases; Male; Mice; Phosphorylation; Protein Binding; Structure-Activity Relationship; Substrate Specificity; Thiadiazoles; Thiazoles; Triazoles	2009

Article

Year

Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.

Journal of medicinal chemistry, 2009, Apr-09, Volume: 52, Issue:7

We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. The compounds are substrate competitive inhibitors that bind to the docking site of the kinase. The reported medicinal chemistry and structure-based optimizations studies resulted in the discovery of selective and potent thiadiazole JNK inhibitors that display promising in vivo activity in mouse models of insulin insensitivity.

Topics: Activating Transcription Factor 2; Animals; Binding Sites; Diabetes Mellitus, Type 2; Drug Design; HeLa Cells; Humans; Hypoglycemic Agents; Insulin Resistance; JNK Mitogen-Activated Protein Kinases; Male; Mice; Phosphorylation; Protein Binding; Structure-Activity Relationship; Substrate Specificity; Thiadiazoles; Thiazoles; Triazoles

2009