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
Rok vydání: 1992
Předmět:
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