Design, synthesis and characterization of lead compounds as anti-inflammatory drugs targeting mPGES-1 via enzymelink screening

Author:

Lu Renzhong1ORCID,Akasaka Hironori1,Ruan Ke-He1ORCID

Affiliation:

1. Department of Pharmacological & Pharmaceutical Sciences, Center for Experimental Therapeutics & Pharmacoinformatics, College of Pharmacy, University of Houston, Houston, TX 77204, USA

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.

Funder

American Heart Association

National Institutes of Health

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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