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Molecules 2018, 23(12), 3232; https://doi.org/10.3390/molecules23123232

Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives

1
Nation Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
2
School of Pharmacy, Anhui Medical University, Hefei 230032, China
3
Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
*
Author to whom correspondence should be addressed.
Received: 7 November 2018 / Revised: 30 November 2018 / Accepted: 3 December 2018 / Published: 7 December 2018
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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. View Full-Text
Keywords: phlorogluciniol; acylphloroglucinol; anti-inflammatory; iNOS; NF-κB phlorogluciniol; acylphloroglucinol; anti-inflammatory; iNOS; NF-κB
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Li, N.; Khan, S.I.; Qiu, S.; Li, X.-C. Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives. Molecules 2018, 23, 3232.

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