Literature DB >> 17466519

Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.

Brian J Lavey1, Joseph A Kozlowski, Bandarpalle B Shankar, James M Spitler, Guowei Zhou, De-Yi Yang, Youheng Shu, Michael K C Wong, Shing-Chun Wong, Neng-Yang Shih, Jie Wu, Stuart W McCombie, Razia Rizvi, Ronald L Wolin, Charles A Lunn.   

Abstract

Structure-activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (CB2) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent CB2 activity, selectivity for CB2 over CB1, and in vivo plasma levels was identified.

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Year:  2007        PMID: 17466519     DOI: 10.1016/j.bmcl.2007.04.028

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


  3 in total

Review 1.  Classification of scaffold-hopping approaches.

Authors:  Hongmao Sun; Gregory Tawa; Anders Wallqvist
Journal:  Drug Discov Today       Date:  2011-10-26       Impact factor: 7.851

Review 2.  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

3.  Hetero-Diels-Alder reaction of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with arylsulfonylcyanides. Synthesis and antimicrobial activity of 4-hydroxy-2-(arylsulfonyl)pyridines.

Authors:  Ibrar Hussain; Mirza Arfan Yawer; Michael Lalk; Ulrike Lindequist; Alexander Villinger; Christine Fischer; Peter Langer
Journal:  Bioorg Med Chem       Date:  2008-10-17       Impact factor: 3.641

  3 in total

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