New furin inhibitors based on weakly basic amidinohydrazones

Bioorg Med Chem Lett. 2011 Jan 15;21(2):836-40. doi: 10.1016/j.bmcl.2010.11.092. Epub 2010 Nov 25.

Abstract

A novel series of amidinohydrazone-derived furin inhibitors was prepared; the most potent compounds 17 and 21 inhibit furin with K(i) values of 0.46 and 0.59μM, respectively. In contrast to inhibitor 17, which still contains a guanidino residue, compound 21 possesses only weakly basic amidinohydrazone groups.

MeSH terms

  • Amidines / chemistry*
  • Amidines / pharmacology*
  • Furin / antagonists & inhibitors*
  • Furin / metabolism*
  • Humans
  • Hydrazones / chemistry*
  • Hydrazones / pharmacology*
  • Molecular Structure

Substances

  • Amidines
  • Hydrazones
  • Furin