Literature DB >> 17884494

New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.

Daniel Pagé1, Hua Yang, William Brown, Christopher Walpole, Manon Fleurent, Meredith Fyfe, François Gaudreault, Stéphane St-Onge.   

Abstract

The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC(50) values. They also showed moderate to good (>350-fold) selectivity over the CB1 receptor.

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Year:  2007        PMID： 17884494     DOI： 10.1016/j.bmcl.2007.09.019

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


  6 in total

1.  CoMFA and CoMSIA analyses on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole derivatives as selective CB2 receptor agonists.

Authors:  Elena Cichero; Sara Cesarini; Luisa Mosti; Paola Fossa
Journal:  J Mol Model       Date:  2010-02-20       Impact factor: 1.810

2.  Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation.

Authors:  Jiaojiao Li; Jing Ji; Ruibo Xu; Zhengfu Li
Journal:  Medchemcomm       Date:  2019-09-17       Impact factor: 3.597

3.  2,3-Dihydro-1-benzofuran derivatives as a series of potent selective cannabinoid receptor 2 agonists: design, synthesis, and binding mode prediction through ligand-steered modeling.

Authors:  Philippe Diaz; Sharangdhar S Phatak; Jijun Xu; Frank R Fronczek; Fanny Astruc-Diaz; Charles M Thompson; Claudio N Cavasotto; Mohamed Naguib
Journal:  ChemMedChem       Date:  2009-10       Impact factor: 3.466

4.  MDA7: a novel selective agonist for CB2 receptors that prevents allodynia in rat neuropathic pain models.

Authors:  M Naguib; P Diaz; J J Xu; F Astruc-Diaz; S Craig; P Vivas-Mejia; D L Brown
Journal:  Br J Pharmacol       Date:  2008-09-01       Impact factor: 8.739

5.  Exploring the effectiveness of novel benzimidazoles as CB2 ligands: synthesis, biological evaluation, molecular docking studies and ADMET prediction.

Authors:  Michele Tonelli; Elena Cichero; Alì Mokhtar Mahmoud; Alessandro Rabbito; Bruno Tasso; Paola Fossa; Alessia Ligresti
Journal:  Medchemcomm       Date:  2018-10-10       Impact factor: 3.597

6.  Tricyclic Pyrazoles. Part 5. Novel 1,4-Dihydroindeno[1,2-c]pyrazole CB2 Ligands Using Molecular Hybridization Based on Scaffold Hopping.

Authors:  Gabriele Murineddu; Battistina Asproni; Stefania Ruiu; Francesco Deligia; Matteo Falzoi; Amedeo Pau; Brian F Thomas; Yanan Zhang; Gérard A Pinna; Luca Pani; Paolo Lazzari
Journal:  Open Med Chem J       Date:  2012-05-17
  6 in total

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