Abstract
Aim: The objective of this study was to synthesize and validate a set of compounds that selectively inhibit mPGES-1, with the potential to be developed into a novel anti-inflammatory drug. Methods: The synthesized compounds were characterized using 1H NMR spectroscopy and LC-MS to confirm their structure. Cellular and enzymatic assays were used to demonstrate their inhibitory activity on prostaglandin E2 production. Results: Docking studies revealed that compounds containing fluoro-, chloro- and methyl- groups displayed strong inhibitory activity against prostaglandin E2. The inhibitory activity of synthesized trimethyl and trifluoro was further validated using enzymatic and cell migration assays. Conclusion: The findings demonstrated that the synthesized compounds possess significant potential as a new generation of nonsteroidal anti-inflammatory drugs that selectively target mPGES-1 with fewer side effects.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 757-767 |
| Number of pages | 11 |
| Journal | Future Medicinal Chemistry |
| Volume | 15 |
| Issue number | 9 |
| DOIs | |
| State | Published - May 1 2023 |
| Externally published | Yes |
Keywords
- anti-inflammation
- COX-2
- COX-2-10aa-mPGES-1
- COX-2-10aa-PGIS
- enzymelink
- microsomal prostaglandin E2 synthase-1
- mPGES-1 inhibitor
- prostacyclin
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery