Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase
| Autor: | Hong-Chi Ho, Gan-Hong Chen, Gialih Lin |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Carbamate
Stereochemistry medicine.medical_treatment Clinical Biochemistry Molecular Conformation Pharmaceutical Science Biochemistry Chemical synthesis Structure-Activity Relationship Reaction rate constant Drug Discovery medicine Animals Horses Molecular Biology Butyrylcholinesterase Cholinesterase biology Chemistry Organic Chemistry Dissociation constant Kinetics Enzyme inhibitor biology.protein Molecular Medicine Epimer Carbamates Cholinesterase Inhibitors |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 8:2747-2750 |
| ISSN: | 0960-894X |
| Popis: | Conformationally restricted carbamate inhibitors, exo -2-norbornyl- N -butylcarbamate ( 1 ), endo -2-norbornyl- N -butylcarbamate ( 2 ), 1-adamantyl- N -butylcarbamate ( 3 ), and 2-adamantyl- N -butylcarbamate ( 4 ) as active site-directed irreversible inhibitors of horse serum butyrylcholinesterase are investigated for values of the dissociation constant ( K I ), the carbamylation constant (k 2 ), and the bimolecular rate constant (k i ). Compound 1 is the most potent inhibitor of the enzyme and the values of K I and k i are 20 nM and 1.1×10 5 M −1 sec −1 . |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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