Literature DB >> 16115769

Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.

Bandarpalle B Shankar1, Brian J Lavey, Guowei Zhou, James A Spitler, Ling Tong, Razia Rizvi, De-Yi Yang, Ronald Wolin, Joseph A Kozlowski, Neng-Yang Shih, Jie Wu, R William Hipkin, Waldemar Gonsiorek, Charles A Lunn.   

Abstract

We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as the groups linking them together, led to sub-nanomolar inhibitors of the CB2 receptor, with high selectivity over CB1.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16115769     DOI: 10.1016/j.bmcl.2005.07.023

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


  4 in total

1.  Endocannabinoids produced upon action potential firing evoke a Cl(-) current via type-2 cannabinoid receptors in the medial prefrontal cortex.

Authors:  Femke S den Boon; Pascal Chameau; Kas Houthuijs; Simone Bolijn; Nicolina Mastrangelo; Chris G Kruse; Mauro Maccarrone; Wytse J Wadman; Taco R Werkman
Journal:  Pflugers Arch       Date:  2014-03-28       Impact factor: 3.657

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

Review 4.  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

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.