Potent transglutaminase inhibitors, dithio β-aminoethyl ketones

Shoichiro Ozaki; Etsuko Ebisui; Kozo Hamada; Akinobu Z Suzuki; Akiko Terauchi; Katsuhiko Mikoshiba

doi:10.1016/j.bmcl.2010.10.136

Potent transglutaminase inhibitors, dithio β-aminoethyl ketones

Bioorg Med Chem Lett. 2011 Jan 1;21(1):377-9. doi: 10.1016/j.bmcl.2010.10.136. Epub 2010 Oct 31.

Authors

Shoichiro Ozaki¹, Etsuko Ebisui, Kozo Hamada, Akinobu Z Suzuki, Akiko Terauchi, Katsuhiko Mikoshiba

Affiliation

¹ Laboratory for Developmental Neurobiology, Brain Development Research Group, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.

PMID: 21134746
DOI: 10.1016/j.bmcl.2010.10.136

Abstract

Potent transglutaminase inhibitors were obtained from disulfide compounds, cystamine, dimethyl cystine, and dimethyl homocystine. The disulfide bond and thiophene ring play an important role in inhibitory activity of synthesized aryl β-amino ketones.

MeSH terms

Disulfides / chemistry
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Ketones / chemical synthesis
Ketones / chemistry*
Ketones / pharmacology
Structure-Activity Relationship
Thiophenes / chemistry
Transglutaminases / antagonists & inhibitors*
Transglutaminases / metabolism

Substances

Disulfides
Enzyme Inhibitors
Ketones
Thiophenes
Transglutaminases