Synthesis and structure activity relationships of glycine amide derivatives as novel Vascular Adhesion Protein-1 inhibitors.

@article{Yamaki2017SynthesisAS,
  title={Synthesis and structure activity relationships of glycine amide derivatives as novel Vascular Adhesion Protein-1 inhibitors.},
  author={S. Yamaki and D. Suzuki and Jiro Fujiyasu and M. Neya and A. Nagashima and M. Kondo and T. Akabane and K. Kadono and Ayako Moritomo and K. Yoshihara},
  journal={Bioorganic \& medicinal chemistry},
  year={2017},
  volume={25 1},
  pages={
          187-201
        }
}
Vascular Adhesion Protein-1 (VAP-1) is a promising therapeutic target for the treatment of several inflammatory-related diseases including diabetic microvascular complication. We identified glycine amide derivative 3 as a novel structure with moderate VAP-1 inhibitory activity. Structure-activity relationship studies of glycine amide derivatives revealed that the tertiary amide moiety is important for stability in rat blood and that the position of substituents on the left phenyl ring plays an… Expand
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  • M. Oja, U. Maran
  • Chemistry, Medicine
  • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2018

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