Literature DB >> 15664857

Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.

Brian J Lavey1, Joseph A Kozlowski, R William Hipkin, Waldemar Gonsiorek, Daniel J Lundell, John J Piwinski, Satwant Narula, Charles A Lunn.   

Abstract

A novel class of cannabinoid CB2 receptor ligands is described. These triaryl bis-sulfones are nanomolar inhibitors of the CB2 receptor and show high selectivity over the cannabinoid CB1 receptor. One example of this new class decreases ligand-induced GTPgammaS binding to recombinant CB2 cell membranes, identifying the compound as a CB2-selective inverse agonist.

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Year:  2005        PMID： 15664857     DOI： 10.1016/j.bmcl.2004.11.007

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


  8 in total

Review 1.  The therapeutic potential of drugs that target cannabinoid receptors or modulate the tissue levels or actions of endocannabinoids.

Authors:  Roger G Pertwee
Journal:  AAPS J       Date:  2005-10-24       Impact factor: 4.009

2.  The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide (SR144528).

Authors:  Evangelia Kotsikorou; Frank Navas; Michael J Roche; Anne F Gilliam; Brian F Thomas; Herbert H Seltzman; Pritesh Kumar; Zhao-Hui Song; Dow P Hurst; Diane L Lynch; Patricia H Reggio
Journal:  J Med Chem       Date:  2013-08-14       Impact factor: 7.446

Review 3.  Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists.

Authors:  C A Lunn; E-P Reich; J S Fine; B Lavey; J A Kozlowski; R W Hipkin; D J Lundell; L Bober
Journal:  Br J Pharmacol       Date:  2007-10-01       Impact factor: 8.739

4.  Sch35966 is a potent, selective agonist at the peripheral cannabinoid receptor (CB2) in rodents and primates.

Authors:  W Gonsiorek; C A Lunn; X Fan; G Deno; J Kozlowski; R W Hipkin
Journal:  Br J Pharmacol       Date:  2007-07-02       Impact factor: 8.739

Review 5.  Endocannabinoid binding to the cannabinoid receptors: what is known and what remains unknown.

Authors:  Patricia H Reggio
Journal:  Curr Med Chem       Date:  2010       Impact factor: 4.530

6.  Site-Selective Suzuki-Miyaura and Sonogashira Cross Coupling Reactions of the Bis(triflate) of 2,4'-Bis(hydroxy)diphenyl Sulfone.

Authors:  Rasheed Ahmad Khera; Asad Ali; Munawar Hussain; Muhammad Farooq Ibad; Alexander Villinger; Peter Langer
Journal:  ChemCatChem       Date:  2012-02-01       Impact factor: 5.686

7.  Cannabinoid receptor type 2 (CB2)-selective N-aryl-oxadiazolyl-propionamides: synthesis, radiolabelling, molecular modelling and biological evaluation.

Authors:  Thomas Rühl; Winnie Deuther-Conrad; Steffen Fischer; Robert Günther; Lothar Hennig; Harald Krautscheid; Peter Brust
Journal:  Org Med Chem Lett       Date:  2012-10-15

8.  First synthesis of 4-(arylsulfonyl)phenols by regioselective [3+3] cyclocondensations of 1,3-bis(silyloxy)-1,3-butadienes with 2-arylsulfonyl-3-ethoxy-2-en-1-ones.

Authors:  Abdolmajid Riahi; Mohanad Shkoor; Olumide Fatunsin; Mathias Lubbe; Helmut Reinke; Peter Langer
Journal:  Tetrahedron Lett       Date:  2008-11-01       Impact factor: 2.415
  8 in total

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