Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists

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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 (IC50= 5 nM). © 2001 Elsevier Science Ltd.

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Link, J. T., Sorensen, B., Liu, G., Pei, Z., Reilly, E. B., Leitza, S., & Okasinski, G. (2001). Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists. Bioorganic and Medicinal Chemistry Letters, 11(8), 973–976. https://doi.org/10.1016/S0960-894X(01)00105-6

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