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Simple synthesis and biological evaluation of flocoumafen and its structural isomers

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Abstract

Simple synthesis and biological properties of flocoumafen 1 and its structural isomers are described. The key synthetic strategies involve Knoevenagel condensation, Grignard reaction, intramolecular ring cyclization and coupling reaction. Flocoumafen 1 was easily separated into cis and trans forms using flash column chromatography. They were then evaluated for suppression of LPS-induced NO generation and anti-excitotoxicity in vitro. It was found that the trans-flocoumafen was potent suppressor of NO generation with the concentration of 10 µM in vitro, while no significant effect for neurotoxicity in cultured cortical neurons.

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Authors and Affiliations

  1. Department of Neuroscience, Ewha Global Challenge, BK21 and Medical Research Institute, School of Medicine, Ewha Womans University, Seoul, 158-710, South Korea

    Jae-Chul Jung, Soyong Jang & Seikwan Oh

  2. Department of Chemistry, Institute for Basic Sciences, College of Natural Sciences, Chungbuk National University, Cheongju, 361-763, Chungbuk, Korea

    Oee-Sook Park

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  1. Jae-Chul Jung
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  2. Soyong Jang
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  3. Seikwan Oh
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  4. Oee-Sook Park
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Correspondence to Oee-Sook Park.

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Jung, JC., Jang, S., Oh, S. et al. Simple synthesis and biological evaluation of flocoumafen and its structural isomers. J Chem Sci 122, 833–838 (2010). https://doi.org/10.1007/s12039-010-0071-2

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  • DOI: https://doi.org/10.1007/s12039-010-0071-2

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