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Structure-activity relationships of benzothiazole GPR35 antagonists.

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.

SUBMITTER: Abdalhameed MM

PROVIDER: S-EPMC5335871 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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Structure-activity relationships of benzothiazole GPR35 antagonists.

Abdalhameed Manahil M MM Zhao Pingwei P Hurst Dow P DP Reggio Patricia H PH Abood Mary E ME Croatt Mitchell P MP

Bioorganic & medicinal chemistry letters 20161205 3

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. ...[more]

PMID: 27989666

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Structure-activity relationships of benzothiazole GPR35 antagonists.

Publications

Structure-activity relationships of benzothiazole GPR35 antagonists.

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