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Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives.

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 µM, respectively, and NF-?B 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.

SUBMITTER: Li N

PROVIDER: S-EPMC6321231 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

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Synthesis and Anti-Inflammatory Activities of Phloroglucinol-Based Derivatives.

Li Ning N Khan Shabana I SI Qiu Shi S Li Xing-Cong XC

Molecules (Basel, Switzerland) 20181207 12

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 ...[more]

PMID: 30544542

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