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Open AccessArticle

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.
Molecules 2018, 23(12), 3232; https://doi.org/10.3390/molecules23123232
Received: 7 November 2018 / Revised: 30 November 2018 / Accepted: 3 December 2018 / Published: 7 December 2018
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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MDPI and ACS Style

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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