Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series

  title={Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series},
  author={William Henry Miller and Fadia E. Ali and William Edward Bondinell and James Francis Callahan and Raul R. Calvo and Drake S. Eggleston and R. Curtis Haltiwanger and William F. Huffman and Hwang Sm and Dalia R. Jakas and Richard M. Keenan and Paul F. Koster and Thomas W. Ku and Chet Kwon and Kenneth A. Newlander and Andrew J. Nichols and Michael F. Parker and James M. Samanen and Linda Sue Southall and Dennis T. Takata and Irene Nijole Uzinskas and Richard E. Valocik and Janice A. Vasko-Moser and Angela S. Wong and Tobias O. Yellin and Catherine C.K. Yuan},
  journal={Bioorganic \& Medicinal Chemistry Letters},
  • W. Miller, F. Ali, C. Yuan
  • Published 5 November 1996
  • Chemistry
  • Bioorganic & Medicinal Chemistry Letters
3 Citations
Progress in the research of GPIIb/IIIa antagonists.
This review covers the recent advances in the development of small RGD (Arg-Gly-Asp sequence) containing peptides and their mimetics as potential antithrombotic agents and expects that newer and more effective nonpeptide mimetics will be developed in the near future.
Fibrinogen receptor antagonists: design and clinical applications.


Conformationally constrained peptides and semipeptides derived from RGD as potent inhibitors of the platelet fibrinogen receptor and platelet aggregation.
The development of both 18 and 22 and the additional structural modifications within the constrained cyclic disulfide ring are described to probe the stereochemical and steric requirements for receptor interaction.
Demonstration of Ac-Arg-Gly-Asp-Ser-NH2 as an antiaggregatory agent in the dog by intracoronary administration.
Ac-RGDS-NH2 is an effective antiplatelet agent after intracoronary administration in the dog and also inhibits collagen-induced platelet aggregation in vitro.
Antithrombotic agents: from RGD to peptide mimetics.
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro.
The cyclic disulfide Ac-cyclo-S,S-[Cys-(N alpha-Me)Arg-Gly-Asp-Pen]-NH2 (SK&F 106760) with improved plasma stability, affinity, and potency constitutes a first potent small peptide entry into the class of novel antithrombotic agents called fibrinogen receptor antagonists.
Reduction of Organic Compounds with NaBH4-Transition Metal Salt Systems. IV. Selective Hydrogenation of Olefines in Unsaturated Esters
Hydrogenation of unsaturated esters was performed with NaBH4-transition metal salt systems. Nickel, cobaltous and cupric salts were effective metal salts for reduction of olefinic esters.