Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors

…, S Ortega-Gutiérrez, I Lastres-Becker…

文献索引：Lopez-Rodriguez; Viso; Ortega-Gutierrez; Lastres-Becker; Gonzalez; Fernandez-Ruiz; Ramos Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4505 - 4508

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被引用次数: 80

摘要

In the present work, we have designed and synthesized a series of arachidonic acid derivatives of general structure I which have been characterized as highly potent and selective inhibitors of anandamide transporter (IC50= 24-0.8 μM, K i> 1000-5000 nM for CB1 and CB2 cannabinoid receptors and vanilloid VR1 receptor). Among them, N-(3-furylmethyl) eicosa-5, 8, 11, 14-tetraenamide deserves special attention as being the most potent ...