Discovery and SAR of Diarylsulfide Cyclopropylamide LFA-1/ICAM-1 Interaction Antagonists.

Abstract Diarylsulfide cyclopropylamides were synthesized and evaluated as LFA-1/ICAM-1 interaction antagonists. A substituent pattern was identified which maximized potency and minimized protein binding as exemplified by antagonist 30 (IC 50 =5 nM).