Fang, Lei and Kraus, Birgit and Lehmann, Jochen and Heilmann, Joerg and Zhang, Yihua and Decker, Michael (2008) Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18 (9). pp. 2905-2909. ISSN 0960-894X, 1464-3405
Full text not available from this repository. (Request a copy)Abstract
Five tacrine-ferulic acid hybrids (6a-e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compounds have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, 6d 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 compounds have, compared to Trolox, high ability to absorb reactive oxygen species. (C) 2008 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | AMYLOID BETA-PEPTIDE; HIGHLY POTENT; OXIDATIVE STRESS; DISEASE; ACETYLCHOLINESTERASE; INHIBITORS; TOXICITY; SITES; LEAD; tacrine; ferulic acid; cholinesterase inhibitor; antioxidant; anti-Alzheimer drug; hybrid molecule |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 03 Nov 2020 07:42 |
| Last Modified: | 03 Nov 2020 07:42 |
| URI: | https://pred.uni-regensburg.de/id/eprint/30923 |
Actions (login required)
 |
View Item |
