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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Bioorganic & medicinal chemistry letters | ||||
| Publisher: | Elsevier | ||||
| Volume: | 18 | ||||
| Number of Issue or Book Chapter: | 9 | ||||
| Page Range: | pp. 2905-2909 | ||||
| Date: | 2008 | ||||
| Additional Information (public): | CAN 149:129007 31-5 Alkaloids 9000-81-1 (Acetylcholinesterase); 9001-08-5 (Cholinesterase) Role: BSU (Biological study, unclassified), BIOL (Biological study) (inhibitors; synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates); 321-64-2 (Tacrine); 1135-24-6 (Ferulic acid) Role: PAC (Pharmacological activity), BIOL (Biological study) (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates); 57165-75-0P; 249290-07-1P; 249290-16-2P; 249290-19-5P; 844874-03-9P Role: PAC (Pharmacological activity), RCT (Reactant), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation), RACT (Reactant or reagent) (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates); 1036298-17-5P; 1036298-18-6P; 1036298-19-7P; 1036298-20-0P; 1036298-21-1P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates); 107-15-3 (1,2-Ethanediamine); 109-76-2 (1,3-Propanediamine); 110-60-1 (1,4-Butanediamine); 373-44-4 (1,8-Octanediamine); 462-94-2 (1,5-Pentanediamine); 537-98-4; 541-41-3; 5396-30-5 Role: RCT (Reactant), RACT (Reactant or reagent) (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates); 62621-20-9P; 1036298-12-0P; 1036298-13-1P; 1036298-14-2P; 1036298-15-3P; 1036298-16-4P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) | ||||
| Identification Number: |
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| Keywords: | Structure-activity relationship (antioxidant synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates) Amines Role: PAC (Pharmacological activity), RCT (Reactant), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation), RACT (Reactant or reagent) (diamines synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates) Alkaloids Role: PAC (Pharmacological activity), RCT (Reactant), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation), RACT (Reactant or reagent) (quinoline synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates) Anti-Alzheimer's agents Cholinesterase inhibitors (synthesis, antioxidant activity, and acetylcholinesterase and butyrylcholinesterase inhibition of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates) tacrine ferulic acid hybrid synthesis cholinesterase inhibitor antioxidant agent anti Alzheimer agent tacrine ferulic acid hydrid | ||||
| Dewey Decimal Classification: | 500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 17239 |
Abstract
Five tacrine-ferulic acid hybrids were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compds. have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, I showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the ...
Abstract
Five tacrine-ferulic acid hybrids were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compds. have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, I showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the peripheral anionic site, whereas a reversible but competitive inhibitory action for butyrylcholinesterase. The antioxidant study revealed that four target compds. have, compared to Trolox, high ability to absorb reactive oxygen species.
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