Literature DB >> 19457667

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

György Szabó1, Róbert Kiss, Dóra Páyer-Lengyel, Krisztina Vukics, Judit Szikra, Andrea Baki, László Molnár, János Fischer, György M Keseru.   

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.

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Year:  2009        PMID: 19457667     DOI: 10.1016/j.bmcl.2009.05.010

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Exploiting the Divalent Nature of Isonitriles: a novel Pictet-Spengler Amidination process.

Authors:  Federico Medda; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2014-05-01       Impact factor: 2.415

Review 2.  Progress in structure based drug design for G protein-coupled receptors.

Authors:  Miles Congreve; Christopher J Langmead; Jonathan S Mason; Fiona H Marshall
Journal:  J Med Chem       Date:  2011-06-15       Impact factor: 7.446

Review 3.  Recent advances in the transition-metal-free synthesis of quinoxalines.

Authors:  Biplob Borah; L Raju Chowhan
Journal:  RSC Adv       Date:  2021-11-19       Impact factor: 4.036

4.  Synthesis and Biological Evaluation of Some [1,2,4]Triazolo[4,3-a]quinoxaline Derivatives as Novel Anticonvulsant Agents.

Authors:  Mohamed Alswah; Adel Ghiaty; Ahmed El-Morsy; Kamal El-Gamal
Journal:  ISRN Org Chem       Date:  2013-09-12

5.  First synthesis of meso-substituted pyrrolo[1,2-a]quinoxalinoporphyrins.

Authors:  Dileep Kumar Singh; Mahendra Nath
Journal:  Beilstein J Org Chem       Date:  2014-04-08       Impact factor: 2.883

  5 in total

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