Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.

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Guckian KM, Lin EY, Silvian L, Friedman JE, Chin D, Scott DM

Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5249-51. doi: 10.1016/j.bmcl.2008.08.061. Epub 2008 Aug 22.

PubMed ID

18778938 [ View in PubMed

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Abstract

A series of meta-substituted anilines were designed and synthesized to inhibit the interaction of LFA-1 with ICAM for the treatment of autoimmune disease. Design of these molecules was performed by utilizing a co-crystal structure for structure-based drug design. The resulting molecules were found to be potent and to possess favorable pharmaceutical properties.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
3-({4-[(1E)-3-morpholin-4-yl-3-oxoprop-1-en-1-yl]-2,3-bis(trifluoromethyl)phenyl}sulfanyl)aniline	Integrin alpha-L	IC 50 (nM)	1.7	N/A	N/A	Details