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<p>Synthesis and evaluation of 2,3,4,9-tetrahydro-1<em>H</em>-carbazole derivatives as selective acetylcholinesterase inhibitors: Potential anti-Alzheimer’s agents</p><p> </p>

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Title Statement <p>Synthesis and evaluation of 2,3,4,9-tetrahydro-1<em>H</em>-carbazole derivatives as selective acetylcholinesterase inhibitors: Potential anti-Alzheimer’s agents</p><p> </p>
 
Added Entry - Uncontrolled Name Kukreja, Hitesh ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Chugh, Rajan ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Singh, Jatinder ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Shah, Ramanpreet ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Singh, Dhandeep ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Singh, Nirmal ; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Chopra, Dimple Sethi; Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala 147 002, India
Singh, Mandeep ; Thapar Institute of Engineering and Technology, Patiala 147 004, India
 
Uncontrolled Index Term Alzheimer’s disease, acetylcholinesterase (AChE), Borsche-Drechsel cyclization reaction, donepzil, 2,3,4,9-tetrahydro-1H-carbazoles
 
Summary, etc. <p>Alzheimer’s disease is an irreversible, progressive brain disorder that slowly destroys memory and cognition skills. Dysfunction of acetylcholine containing neurons in the brain contributes substantially to the cognitive decline observed in Alzheimer's disease. Hence, our focus is to synthesize cholinesterase inhibitors. A series (22 compounds) of 6- and 9-substituted derivatives of 2,3,4,9-tetrahydro-1<em>H</em>-carbazole have been prepared and <em>in vitro</em> evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by Ellman’s method. By comparing selectivity with standard drug donepezil, amino derivative <strong>3</strong>, methylamino derivative <strong>4</strong> and butyl nitro derivative <strong>17</strong> have been found to be selective AChE inhibitors. Borsche-Drechsel cyclization reaction has been carried out to synthesize 2,3,4,9-tetrahydrocarbazole ring followed by nitration, reduction and derivative synthesis.</p><p> </p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry -Section B (IJC-B)
2021-01-20 16:29:04
 
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http://op.niscair.res.in/index.php/IJCB/article/view/32397
 
Data Source Entry Indian Journal of Chemistry -Section B (IJC-B); ##issue.vol## 60, ##issue.no## 01 (2021): Indian Journal of Chemistry Section - B (IJCB)
 
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Nonspecific Relationship Entry http://op.niscair.res.in/index.php/IJCB/article/download/32397/465500101
 
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