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Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Mar 01; Vol. 20 (5), pp. 1721-3. Date of Electronic Publication: 2010 Jan 20. - Publication Year :
- 2010
-
Abstract
- We synthesized carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives 3a-u and evaluated their anti-cholinesterase activities. In vitro evaluation showed that cyclohexylmethylcarbamate derivative 3u potently and selectively inhibits butyrylcholinesterase.<br /> (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Acetylcholinesterase chemistry
Acetylcholinesterase metabolism
Butyrylcholinesterase metabolism
Cholinesterase Inhibitors chemistry
Cholinesterase Inhibitors pharmacology
Drug Design
Humans
Neuroprotective Agents chemistry
Neuroprotective Agents pharmacology
Physostigmine chemical synthesis
Physostigmine chemistry
Physostigmine pharmacology
Structure-Activity Relationship
Butyrylcholinesterase chemistry
Carbamates chemistry
Cholinesterase Inhibitors chemical synthesis
Neuroprotective Agents chemical synthesis
Physostigmine analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20137941
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.01.035