2. Academic Validation
  3. Structure-activity relationships of benzothiazole GPR35 antagonists

Structure-activity relationships of benzothiazole GPR35 antagonists

  • Bioorg Med Chem Lett. 2017 Feb 1;27(3):612-615. doi: 10.1016/j.bmcl.2016.12.012.
Manahil M Abdalhameed 1,  Pingwei Zhao 2,  Dow P Hurst 1,  Patricia H Reggio 3,  Mary E Abood 4,  Mitchell P Croatt 5
Affiliations

Affiliations

  • 1 Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
  • 2 Department of Anatomy and Cell Biology and Center for Substance Abuse Research, Temple University, Philadelphia, PA 19140, United States.
  • 3 Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States. Electronic address: [email protected].
  • 4 Department of Anatomy and Cell Biology and Center for Substance Abuse Research, Temple University, Philadelphia, PA 19140, United States. Electronic address: [email protected].
  • 5 Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States. Electronic address: [email protected].
PMID: 27989666 DOI: 10.1016/j.bmcl.2016.12.012
Abstract

The first structure-activity relationships for a benzothiazole scaffold acting as an antagonist at GPR35 is presented. Analogues were designed based on a lead compound that was previously determined to have selective activity as a GPR35 antagonist. The synthetic route was modular in nature to independently explore the role of the middle and both ends of the scaffold. The activities of the analogues illustrate the importance of all three segments of the compound.

Keywords

Antagonist; Benzothiazole; G protein-coupled receptor; GPR35; SAR.

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