Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core.

ABSTRACT: We present the development of conformationally pre-organised Dyrk1A inhibitors based on the hydroxybenzothiazole urea scaffold. The modifications introduced to the discovered hit (AHS-211) proved the crucial role of the urea linker to preserve the bioactive conformation and led to the development of compound b5 as a promising selective Dyrk1A inhibitor.

SUBMITTER: Salah M 

PROVIDER: S-EPMC6071757 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature