Hit-to-lead optimization of pyrrolo [1, 2-a] quinoxalines as novel cannabinoid type 1 receptor antagonists

…, K Vukics, J Szikra, A Baki, L Molnár, J Fischer…

Index: Szabo, Gyoergy; Kiss, Robert; Payer-Lengyel, Dora; Vukics, Krisztina; Szikra, Judit; Baki, Andrea; Molnar, Laszlo; Fischer, Janos; Keseru, Gyoergy M. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 13 p. 3471 - 3475

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Citation Number: 25

Abstract

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.