Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors

AuthorMehdi Valipouren
AuthorIssa Davajien
AuthorNiusha Abedien
AuthorMahsa Rajabien
AuthorTuba Tüylü Küçükkılınçen
AuthorBeyza Ayazgöken
AuthorHamid Irannejaden
Issued Date2019-07-31en
AbstractAlzheimer’s disease (AD) is a neuroinflammatory based pathologic state in which β-amyloid aggregates are major devastating agents. In this study, a series of 2-hydroxyiminoethanones were synthesized and evaluated as anti-inflammatory in carrageenan and formalin tests and inhibitors of β-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more β-amyloid disaggregation ability than reference drugs rifampicin and donepezil and compound 2b was the best compound in this series and could reduce the extent of amyloid aggregation to 50.9%. Interestingly, compounds 1b and 3b showed significant anti-inflammatory activity in carrageenan-induced paw edema compared to control group and equivalent to the reference drug indomethacin. 2-Hydeoxyiminoethanones are privileged scaffold for further drug research and development as anti-neuroinflammatory and neuroprotective agents.en
DOIhttps://doi.org/10.22037/ijpr.2019.15567.13181en
KeywordSynthesisen
KeywordAnti- inflammatoryen
KeywordAlzheimer′s diseaseen
Keywordhydroxyiminoethanoneen
Keywordβ-amyloid aggregationen
PublisherBrieflandsen
TitleSynthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitorsen
TypeOriginal Articleen

Files

Original bundle

Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
ijpr-18-1288.pdf
Size:
791.76 KB
Format:
Adobe Portable Document Format
Description:
Article/s PDF