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

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.

A series of novel sulfonyl- and phosphonyl amidine anti-bone resorptive agents were developed. The structure–activity relationships are described.Figure optionsDownload as PowerPoint slide