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Hit-to-lead Optimization of Pyrrolo[1,2-a]quinoxalines as Novel Cannabinoid Type 1 Receptor Antagoni

Hit-to-lead Optimization of Pyrrolo[1,2-a]quinoxalines as Novel Cannabinoid Type 1 Receptor Antagoni

  1. helikophis
    Hit-to-lead optimization of a novel series of N-alkyl-N-[2-oxo-2-(4-aryl-4H-pyrrolo[1,2-a]quinoxaline-5-yl)-ethyl]-carboxylic acid amides, derived from a high throughput screening (HTS) hit, are described. Subsequent optimization led to identification of in vitro potent cannabinoid 1 receptor (CB1R) antagonists representing a new class of compounds in this area.