Girisha, H. R. and Narendra Sharath Chandra, J. N. and Boppana, Sriramamurthy and Malviya, Manish and Sadashiva, C. T. and Rangappa, K. S. (2009) Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase. European Journal of Medicinal Chemistry, 44 (10). pp. 4057-4062. ISSN 1768-3254
Full text not available from this repository. (Request a copy)Abstract
Hypocholinergic function associated with Alzheimer's disease (AD) is well-accepted hypothesis, in this regard, many research attempts have been made to elevate the reduced cholinergic neurotransmission, among them two main treatment strategies were widely explored, namely stimulation of muscarinic receptor 1 and/or reversible inhibition of acetylcholinesterase (AChE) enzyme. In an attempt to improve the efficacy and to minimize general side effects of these ACNE inhibitors, many lead molecules are developed in research; one among them is piperidine derivative. Donazepil is a widely prescribed ACNE inhibitor which displays a piperidine ring in its structure. In the present study, we have docked cis-2,6-dimethyl piperidine sulfonamides (3a-i) on ACNE enzyme and synthesized by nucleophilic substitution reaction between cis-2,6-dimethyl piperidine and alkyl/aryl sulfonyl chlorides in the presence of triethylamine. These piperidine sulfonamides were subjected to in vitro AChE enzyme inhibition studies and in vivo antiamnesic study to reverse scopolamine induced memory loss in rats. Two derivatives (3a and f) in this class of piperidines (3a-i) showed considerable inhibition against different sources of ACNE in vitro and reduced average number of mistakes done by wistar rats as compared to scopolamine treated group in vivo (rodent memory evaluation). (C) 2009 Published by Elsevier Masson SAS.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Alzheimer's diseases; AChE; Docking |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 17 Aug 2019 10:33 |
| Last Modified: | 19 Dec 2020 05:22 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6691 |
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