Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives

Authors

• Ning Li, University of Mississippi; Anhui Medical University
• Shabana I. Khan, University of Mississippi
• Shi Qiu, University of Mississippi
• Xing-Cong Li, University of Mississippi

Department

Pharmacy

Document Type

Article

DOI

10.3390/molecules23123232

Publication Date

12-7-2018

Abstract

The natural product phloroglucinol-based derivatives representing monoacyl-, diacyl-, dimeric acyl-, alkylated monoacyl-, and the nitrogen-containing alkylated monoacylphloro- glucinols were synthesized and evaluated for inhibitory activities against the inflammatory mediators such as inducible nitric oxide synthase (iNOS) and nuclear factor kappaB (NF-κB). The diacylphloroglucinol compound 2 and the alkylated acylphloroglucinol compound 4 inhibited iNOS with IC50 values of 19.0 and 19.5 µM, respectively, and NF-κB with IC50 values of 34.0 and 37.5 µM, respectively. These compounds may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.

Relational Format

journal article

Recommended Citation

Li, N., Khan, S. I., Qiu, S., & Li, X.-C. (2018). Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives. Molecules, 23(12), 3232. https://doi.org/10.3390/molecules23123232

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