Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.
@article{Keenan1999ConformationalPI, title={Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.}, author={Richard M. Keenan and James Francis Callahan and James M. Samanen and William Edward Bondinell and Raul R. Calvo and L Chen and Charles W. Debrosse and Drake S. Eggleston and R. Curtis Haltiwanger and S. M. Hwang and Dalia R. Jakas and Thomas W. Ku and William Henry Miller and Kenneth A. Newlander and Andrew J. Nichols and Michael F. Parker and L S Southhall and Irene Nijole Uzinskas and Janice A. Vasko-Moser and Joseph W. Venslavsky and Angela S. Wong and William F. Huffman}, journal={Journal of medicinal chemistry}, year={1999}, volume={42 4}, pages={ 545-59 } }
Previously, we reported the direct design of highly potent nonpeptide 3-oxo-1,4-benzodiazepine fibrinogen receptor antagonists from a constrained, RGD-containing cyclic semipeptide. The critical features incorporated into the design of these nonpeptides were the exocyclic amide at the 8-position which overlaid the Arg carbonyl, the phenyl ring which maintained an extended Gly conformation, and the diazepine ring which mimicked the gamma-turn at Asp. In this paper, we investigate conformational…
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