Structure-activity relationships of benzothiazole GPR35 antagonists

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• 作者：Manahil M. Abdalhameed^a ; Pingwei Zhao^b ; Dow P. Hurst^a ; Patricia H. Reggio^a ; ^{phreggio@uncg.edu} ; Mary E. Abood^b ; ^{mabood@temple.edu} ; Mitchell P. Croatt^a ; ^{mpcroatt@uncg.edu}
• 关键词：GPR35 ; Antagonist ; G protein-coupled receptor ; Benzothiazole ; SAR
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：27
• 期：3
• 页码：612-615
• 全文大小：1355 K
• 卷排序：27

文摘

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.