5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.

@article{BartolomNebreda19995Tryptophylamino13dioxoper,
  title={5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.},
  author={J. Bartolom{\'e}-Nebreda and I. Gomez-Monterrey and M. Garc{\'i}a-L{\'o}pez and R. Gonz{\'a}lez-Mu{\~n}iz and M. Mart{\'i}n-Mart{\'i}nez and S. Ballaz and E. Cenarruzabeitia and M. Latorre and J. del R{\'i}o and R. Herranz},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 22},
  pages={
          4659-68
        }
}
Analogues of the previously reported potent and highly selective CCK(1) receptor antagonist (4aS, 5R)-2-benzyl-5-(N-Boc-tryptophyl)amino-1,3-dioxoperhydropyrido-[1, 2-c]pyrimidine (2a) were prepared to explore the structural requirements at the Boc-tryptophan domain for CCK(1) receptor affinity. Structural modifications of 2a involved the Trp side chain, its conformational freedom, the Boc group, and the carboxamide bond. Results of the CCK binding and in vitro functional activity evaluation… Expand

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