Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives

Molecules

Shi Qiu¹  Xing-Cong Li¹  Ning Li¹  ShabanaI. Khan¹ 

[1] Nation Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA;

关键词: phlorogluciniol;    acylphloroglucinol;    anti-inflammatory;    iNOS;    NF-κB;   

DOI  :  10.3390/molecules23123232

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown