(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: Synthesis, in vitro, in vivo, and X-ray crystallographic characterization

A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.

Graphical abstractPotency, selectivity, and pharmacokinetic properties of DPP-IV inhibitors developed from a HTS hit were optimized resulting in the identification of a pre-clinical candidate for further profiling.Figure optionsDownload full-size imageDownload as PowerPoint slide