Synthesis and In Vitro Anti-Inflammatory Activity of Pyrrolo[1,2-A]pyrazines via Pd-Catalyzed Intermolecular Cyclization Reaction

Yan Mei Zhou; Yong Wei; Jin Yang; Hai Hai Li; Miao Deng Liu; Nian Yu Huang

doi:10.4028/www.scientific.net/AMR.830.115

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HomeAdvanced Materials ResearchAdvanced Materials Research Vol. 830Synthesis and In Vitro Anti-Inflammatory Activity...

Synthesis and In Vitro Anti-Inflammatory Activity of Pyrrolo[1,2-A]pyrazines via Pd-Catalyzed Intermolecular Cyclization Reaction

Abstract:

Pyrrolo [1,2-a] pyrazine possessed widely bioactivities due to its particular structure. In this work, three pyrrolo [1,2-a] pyrazines derivatives were synthesized from the 2-bromo-5-methoxypyrazine and propargyl amines or ethers through the Pd-catalyzed intermolecular cycloisomerization strategy. Their structures were characterized by NMR, IR, EI-MS and elemental analysis, and all of them exhibited moderate in vitro anti-inflammatory effects with the inhibitions of 43-59% against IL-6 at 50 μM. The compound 3c revealed relatively good anti-inflammatory activities. The bioactive pyrrolo [1,2-a] pyrazines might be potentially used as anti-inflammatory agents.

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Periodical:

Advanced Materials Research (Volume 830)

Pages:

115-118

DOI:

https://doi.org/10.4028/www.scientific.net/AMR.830.115

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Online since:

October 2013

Authors:

Yan Mei Zhou, Yong Wei, Jin Yang, Hai Hai Li, Miao Deng Liu, Nian Yu Huang*

Keywords:

Anti-Inflammatory Agents, IL-6 Inhibitory Activity, Intermolecular Cyclization, Pyrrolo[1,2-a]pyrazine, Synthesis

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* - Corresponding Author

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