Pyrrolo[2,3-c]azepine derivatives: A new class of potent protein tyrosine phosphatase 1B inhibitors

A series of pyrrolo[2,3-c]azepine derivatives was designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B (PTP1B) in vitro. The results demonstrated that compounds bearing a biphenyl moiety were proved to markedly influence the potency of these inhibitors. Particularly, compounds 29, 35 and 36 showed interesting inhibition with IC50 value of 16.36, 14.93 and 13.92 μM, respectively.

Graphical abstractA series of pyrrolo[2,3-c]azepine derivatives were prepared and evaluated as PTP1B inhibitors. The 1-biphenyl substituted compounds exhibited the most potent inhibitory activity, the best of which has an IC50 value of 13.92 μM in vitro (compound 36).Figure optionsDownload full-size imageDownload as PowerPoint slide