A series of twenty-five derivatives of tetrahydro-β-carbolines 1-3 was synthesized and assayed on FAAH and TRPV1 and TRPA1 channels. Four carbamates, that is, 5a,c,e, and 9b inhibited FAAH with significant potency and interacted also effectively with TRPV1 and TRPA1 nociceptive receptors, while ureas 7b,d,f, and 8a,b were endowed with specific submicromolar TRPV1 modulating activities.
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【Tetrahydro-β-carboline derivatives targeting fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channels.].
【靶向脂肪酸酰胺水解酶 (FAAH) 和瞬时受体电位 (TRP) 通道的四氢-β-carboline衍生物。】
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DOI：10.1016/j.bmcl.2012.10.137文章类型：杂志文章
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合成了一系列25种四氢-β-carbolines 1-3衍生物，并在FAAH和TRPV1和TRPA1通道上进行了测定。四种氨基甲酸酯，即5a，c，e和9b以显着的效力抑制FAAH，并且还与TRPV1和TRPA1伤害性受体有效相互作用，而ureas 7b，d，f和8a，b具有特定的亚微摩尔TRPV1调节活性。
