N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.

Medicinal Chemistry

Abstract

A series of 1,3,5-triazine-2,4,6-triamines were prepared and analyzed as inhibitors of glucocerebrosidase. Synthesis, structure activity relationships and the selectivity of chosen analogues against related sugar hydrolases enzymes are described.

Authors

Huang, Wenwei; Zheng, Wei; Urban, Daniel J; Inglese, James; Sidransky, Ellen; Austin, Christopher; Thomas, Craig;

Keywords

  • Enzyme Inhibitors/ chemistry
  • Enzyme Inhibitors/ pharmacology
  • Gaucher Disease/ enzymology
  • Glucosylceramidase/ antagonists & inhibitors
  • Humans
  • Triazines/ chemistry
  • Triazines/ pharmacology

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