1. Effect of novel N-arylurea- substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer’s dementia models
- Author
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N. R. Thimmegowda, M.N. Subhash, Kanchugarakoppal S. Rangappa, C. V. Kavitha, Manish Malviya, Y.C. Sunil Kumar, and J. N. Narendra Sharath Chandra
- Subjects
Sulfonyl ,chemistry.chemical_classification ,Stereochemistry ,Organic Chemistry ,Muscarinic acetylcholine receptor M1 ,Muscarinic agonist ,chemistry.chemical_compound ,chemistry ,Morpholine ,Muscarinic acetylcholine receptor ,medicine ,Moiety ,Structure–activity relationship ,Arecoline ,medicine.drug - Abstract
A series of novel, potent, and selective muscarinic receptor 1 agonists (M1 receptor agonists) that employ a key N-substituted morpholine Arecoline moiety has been synthesized as part of research effort for the therapy of Alzheimer's diseases. The ester group of arecoline (which is reported as muscarinic agonist) has been replaced by N-substituted morpholine ring. The structure activity relationship reveals that the electron donating 4-substituted sulfonyl derivatives (9a, 9b, 9c, and 9e) on the nitrogen atom of the morpholine ring increases the affinity of M1 receptor binding 50- to 80-fold greater than the corresponding arecoline. Other derivatives also showed considerable M1 receptor binding affinity. (C) 2008 Elsevier Ltd. All rights reserved.
- Published
- 2008
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