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Trienomycin A-simplified analogs: Synthesis and anti-neuroinflammatory activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2023 Jan 15; Vol. 80, pp. 129122. Date of Electronic Publication: 2022 Dec 30. - Publication Year :
- 2023
-
Abstract
- A series of novel trienomycin A (TA)-mimetic compounds (5a-p) have been designed, synthesized, and evaluated for their in vitro anti-neuroinflammatory and neuroprotective activities. Among them, compounds 5h, 5n, and 5o exhibits relatively strong NO inhibitory activity in LPS-activated BV-2 cells with the EC <subscript>50</subscript> values of 12.4, 17.3, and 8.9 μM, respectively. Moreover, 5h showed evidently neuroprotective effect against H <subscript>2</subscript> O <subscript>2</subscript> -induced PC-12 cells without cytotoxicity at 20 μM. Overall, these compounds can provide a better understanding of the structure-activity relationship of TA and furnish research ideas for anti-neuroinflammatory and neuroprotective agents.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2022 Elsevier Ltd. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 80
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 36592870
- Full Text :
- https://doi.org/10.1016/j.bmcl.2022.129122