Literature DB >> 27989666

Structure-activity relationships of benzothiazole GPR35 antagonists.

Manahil M Abdalhameed1, Pingwei Zhao2, Dow P Hurst1, Patricia H Reggio3, Mary E Abood4, Mitchell P Croatt5.   

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.
Copyright © 2016. Published by Elsevier Ltd.

Entities:  

Keywords:  Antagonist; Benzothiazole; G protein-coupled receptor; GPR35; SAR

Mesh：

Substances：

Year:  2016        PMID： 27989666      PMCID： PMC5335871          DOI： 10.1016/j.bmcl.2016.12.012

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


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