N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.

Basic Information

ID: ALA1145733

Journal: Bioorg Med Chem Lett

Title: N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.

Authors: Doherty GA, Yang GX, Borges E, Tong S, McCauley ED, Treonz KM, Van Riper G, Pacholok S, Si Q, Koo GC, Shah K, Mumford RA, Hagmann WK.

Abstract: A series of isonicotinoyl-(L)-aminophenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. These compounds exhibit subnanomolar binding affinity to VLA-4 and significant off-rates. The interplay between off-rate, protein binding and pharmacokinetics is discussed.

CiteXplore: 12749892

DOI: 10.1016/s0960-894x(03)00308-1

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