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Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives

Author:
Li, Ning, Khan, Shabana, Qiu, Shi, Li, Xing-Cong
Source:
Molecules 2018 v.23 no.3232 pp. 1-8
ISSN:
1420-3049
Subject:
anti-inflammatory activity, anti-inflammatory agents, inducible nitric oxide synthase, inhibitory concentration 50, synthesis, transcription factor NF-kappa B
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-B). The diacylphloroglucinol compound 2 and the alkylated acylphloroglucinol compound 4 inhibited iNOS with IC50 values of 19.0 and 19.5 M, respectively, and NF-B with IC50 values of 34.0 and 37.5 M, respectively. These compounds may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.
Agid:
6471202
Handle:
10113/6471202