.ALPHA.-Glucosidase Inhibitors with a Phthalimide Skeleton. Structure-Activity Relationship Study.

Alpha glucosidase inhibitors.

Alpha glucosidase inhibitors (AGIs) are a unique class of anti-diabetic drugs. Derived from bacteria, these oral drugs are enzyme inhibitors which do not have a pancreato -centred mechanism of action. Working to delay carbohydrate absorption in the gastrointestinal tract, they control postprandial hyperglycaemia and provide unquestioned cardiovascular benefit. Specially suited for a traditional...

Alpha-glucosidase inhibitors with a 4,5,6,7-tetrachlorophthalimide skeleton pendanted with a cycloalkyl or dicarba-closo-dodecaborane group.

Previous studies of alpha-glucosidase inhibitors derived from thalidomide revealed that 4,5,6,7-tetrachloro-N-alkylphthalimide derivatives are superior lead compounds. Structure-activity relationship studies indicated that a hydrophobic group at the N(2) position is mandatory for potent activity. Accordingly, we have designed and synthesized some 4,5,6,7-tetrachloro-N-cycloalkylphthalimide and ...

a structure–activity relationship survey of histone deacetylase (hdac) inhibitors

a quantitative structure-activity relationship (qsar) study of some diaryl urea derivatives of b-raf inhibitors

in the current study, both ligand-based molecular docking and receptor-based quantitative structure activity relationships (qsar) modeling were performed on 35 diaryl urea derivative inhibitors of v600e b-raf. in this qsar study, a linear (multiple linear regressions) and a nonlinear (partial least squares least squares support vector machine (pls-ls-svm)) were used and compared. the predictive...

Structure–Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors

EPAC proteins are therapeutic targets for the potential treatment of cardiac hypertrophy and cancer metastasis. Several laboratories use a tetrahydroquinoline analog, CE3F4, to dissect the role of EPAC1 in various disease states. Here, we report SAR studies with tetrahydroquinoline analogs that explore various functional groups. The most potent EPAC inhibitor 12a exists as a mixture of insepara...