Xuehong Luo

Publications (3)11.16 Total impact

• Article: γ-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.

  Yun-Xing Cheng, Mehrnaz Pourashraf, Xuehong Luo, Sanjay Srivastava, Christopher Walpole, Dominic Salois, Stephane St-Onge, Kemal Payza, Etienne Lessard, Xiao Hong Yu, Mirosław J Tomaszewski
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  ABSTRACT: An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
  Bioorganic & medicinal chemistry letters 02/2012; 22(4):1619-24. · 2.65 Impact Factor
• Article: Practical synthesis of quinoxalinones via palladium-catalyzed intramolecular N-arylations.

  Xuehong Luo, Etienne Chenard, Peter Martens, Yun-Xing Cheng, Mirosław J Tomaszewski
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  ABSTRACT: A practical and highly efficient route to the synthesis of pharmaceutically interesting quinoxalinone scaffolds is reported. The key step involves an intramolecular palladium-catalyzed N-arylation under microwave irradiation. The developed methodology tolerates a variety of bromoanilides to afford a diverse collection of bicyclic and polycyclic quinoxalinones in high yield.
  Organic Letters 08/2010; 12(16):3574-7. · 5.86 Impact Factor
• Article: Novel benzimidazole derivatives as selective CB2 agonists.

  Daniel Pagé, Elise Balaux, Luc Boisvert, Ziping Liu, Claire Milburn, Maxime Tremblay, Zhongyong Wei, Simon Woo, Xuehong Luo, Yun-Xing Cheng, [......], Fei Zhou, William Brown, Miroslaw Tomaszewski, Christopher Walpole, Leila Hodzic, Stéphane St-Onge, Claude Godbout, Dominic Salois, Kemal Payza, Keymal Payza
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  ABSTRACT: The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.
  Bioorganic & medicinal chemistry letters 07/2008; 18(13):3695-700. · 2.65 Impact Factor