Bioorganic and Medicinal Chemistry Letters p. 279 - 284 (1999)
Update date:2022-07-29
Topics:
Elliott, John T.
Hoekstra, William J.
Maryanoff, Bruce E.
Prestwich, Glenn D.
Photoactivatable analogs of the human thrombin receptor (PAR-1) antagonist, N-trans-cinnamoyl-p-fluoroPhe-p-guandinoPhe-Leu-Arg-NH2 (BMS- 197525), were prepared with benzophenone substitutions in the N-terminal, Leu, or Arg position. The analogs retained antagonist activity (with reduced potency); the tritium-labeled isotopomers are potential photoaffinity labels for the receptor. C-Terminal extension of the analogs with ornithine(biotin) did not significantly alter antagonist potency.
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