Design, synthesis and biological evaluation of GPR55 agonists.

Journal Article (Journal Article)

GPR55, a G protein-coupled receptor, is an attractive target to alleviate inflammatory and neuropathic pain and treat osteoporosis and cancer. Identifying a potent and selective ligand will aid to further establish the specific physiological roles and pharmacology of the receptor. Towards this goal, a targeted library of 22 compounds was synthesized in a modular fashion to obtain structure-activity relationship information. The general route consisted of coupling a variety of p-aminophenyl sulfonamides to isothiocyanates to form acylthioureas. For the synthesis of a known naphthyl ethyl alcohol motif, route modification led to a shorter and more efficient process. The 22 analogues were analyzed for their ability to serve as agonists at GPR55 and valuable information for both ends of the molecule was ascertained.

Full Text

Duke Authors

Cited Authors

  • Fakhouri, L; Cook, CD; Al-Huniti, MH; Console-Bram, LM; Hurst, DP; Spano, MBS; Nasrallah, DJ; Caron, MG; Barak, LS; Reggio, PH; Abood, ME; Croatt, MP

Published Date

  • August 15, 2017

Published In

Volume / Issue

  • 25 / 16

Start / End Page

  • 4355 - 4367

PubMed ID

  • 28673732

Pubmed Central ID

  • PMC5752104

Electronic International Standard Serial Number (EISSN)

  • 1464-3391

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2017.06.016


  • eng

Conference Location

  • England