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Design, synthesis and biological evaluation of GPR55 agonists.
Fakhouri, Lara; Cook, Christopher D; Al-Huniti, Mohammed H; Console-Bram, Linda M; Hurst, Dow P; Spano, Michael B S; Nasrallah, Daniel J; Caron, Marc G; Barak, Larry S; Reggio, Patricia H; Abood, Mary E; Croatt, Mitchell P.
Affiliation
  • Fakhouri L; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Cook CD; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Al-Huniti MH; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Console-Bram LM; Temple University School of Medicine, Anatomy and Cell Biology, Center for Substance Abuse Research, 3420 North Broad St., Philadelphia, PA 19140, United States.
  • Hurst DP; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Spano MBS; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Nasrallah DJ; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Caron MG; Duke Center of Excellence, 444 Sands Building, Department of Cell Biology, Durham, NC 27710, United States.
  • Barak LS; Duke Center of Excellence, 444 Sands Building, Department of Cell Biology, Durham, NC 27710, United States.
  • Reggio PH; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • Abood ME; Temple University School of Medicine, Anatomy and Cell Biology, Center for Substance Abuse Research, 3420 North Broad St., Philadelphia, PA 19140, United States.
  • Croatt MP; Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States. Electronic address: mpcroatt@uncg.edu.
Bioorg Med Chem ; 25(16): 4355-4367, 2017 08 15.
Article in En | MEDLINE | ID: mdl-28673732
ABSTRACT
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiourea / Drug Design / Receptors, G-Protein-Coupled Limits: Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Document type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiourea / Drug Design / Receptors, G-Protein-Coupled Limits: Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Document type: Article Affiliation country: United States