Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5
Autor: | Susan Fisher, Anthony Jerome Thomas, Sharie L. Myers, Michael R. Pavia, Walter H. Moos, Kathryn B. Sanders, Robert E. Davis, Linda L. Coughenour |
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Rok vydání: | 1992 |
Předmět: |
chemistry.chemical_classification
Ketone Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Muscarinic acetylcholine receptor M1 Oxime Biochemistry Muscarinic agonist In vitro chemistry.chemical_compound Drug Discovery Muscarinic acetylcholine receptor Oxotremorine medicine Molecular Medicine Cholinergic Molecular Biology medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 2:803-808 |
ISSN: | 0960-894X |
Popis: | There is considerable interest in muscarinic acetylcholine receptor (mAChR) subtype selective agents as cholinomimetics for the treatment of senile dementia of the Alzheimer's type (SDAT). A series of substituted analogs similar to the muscarinic agonists UH5 and UH28 (analogs of the muscarinic agonist oxotremorine) were synthesized and evaluated pharmacologically. Several oxime analogues of UH5 demonstrate agonist-like properties in vitro at muscarinic receptors. One oxime in this series (Compound 18) was found to be almost five fold more m1 selective than UH5. |
Databáze: | OpenAIRE |
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