Bioorganic and Medicinal Chemistry Letters p. 81 - 86 (1996)
Update date:2022-08-05
Topics:
Sall, Daniel J.
Arfsten, Ann E.
Berry, Dennis R.
Denney, Michael L.
Harms, Cathy S.
McCowan, Jefferson R.
Ray, Judith K.
Scarborough, Robert M.
Um, Suzane L.
Utterback, Barbara G.
Jakubowski, Joseph A.
A series of substituted amidinoindoles have been prepared as mimics of the RGD sequence and were studied as antagonists of the platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa). The agents were potent and selective antagonists of GPIIb-IIIa. Compared to their acyclic counterparts, the amidinoindole series bound with 10- to 20-fold greater affinity, indicating the advantages of added conformational restriction and/or hydrophobicity in the basic region of RGD mimics.
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