Synthesis and SAR of sulfonyl- and phosphoryl amidine compounds as anti-resorptive agents

Bioorg Med Chem Lett. 2010 Jan 15;20(2):541-5. doi: 10.1016/j.bmcl.2009.11.104. Epub 2009 Nov 26.

Abstract

Sulfonyl amidines (1) and phosphoryl amidines (2), which were efficiently synthesized via a Cu-catalyzed one pot reaction, showed potent anti-bone resorptive activity in vitro. Structure activity relationship studies led to the identification of numerous osteoclast differentiation inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acid Phosphatase / metabolism
  • Amidines / chemical synthesis*
  • Amidines / chemistry
  • Amidines / pharmacology
  • Animals
  • Catalysis
  • Copper / chemistry
  • Isoenzymes / metabolism
  • Mice
  • Organophosphonates / chemistry*
  • Osteoclasts / drug effects
  • Structure-Activity Relationship
  • Sulfones / chemistry*
  • Tartrate-Resistant Acid Phosphatase

Substances

  • Amidines
  • Isoenzymes
  • Organophosphonates
  • Sulfones
  • Copper
  • Acid Phosphatase
  • Tartrate-Resistant Acid Phosphatase