Effect of novel N-aryl sulfonamide substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer’s dementia models

Sunil Kumar, Y. C. and Malviya, Manish and Narendra Sharath Chandra, J. N. and Sadashiva, C. T. and Ananda Kumar, C. S. and Benaka Prasad, S. B. and Prasanna, D. S. and Subhash, M. N. and Rangappa, K. S. (2008) Effect of novel N-aryl sulfonamide substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer’s dementia models. Bioorganic & Medicinal Chemistry, 16 (9). 5157 - 5163. ISSN 1464-3391

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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 The ester group of arecoline (which is reported as muscarinic agonist) has been replaced by N-substituted morpholine ring.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.

Item Type:	Article
Uncontrolled Keywords:	Alzheimer’s diseases, M1 agonists, Morpholino arecolines, Displacement assay, Rat brain, In vitro, In vivo
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Manjula P Library Assistant
Date Deposited:	22 Aug 2019 07:41
Last Modified:	22 Aug 2019 07:41
URI:	http://eprints.uni-mysore.ac.in/id/eprint/6887

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