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(a) For PAR-2: Nystedt, S., Emilsson, K., Wahlestedt, C., Sundelin, J. Proc. Natl. Acad Sci. U.S.A. 1994, 91, 9208. Nystedt, S.; Emilsson, K.; Larsson, A.-K.; Stroembeck, B.; Sundelin, J. Eur. J. Biochem. 1995, 232, 84. Nystedt, S.; Larsson, A.-K.; Aberg, H.; Sundelin, J. J. Biol. Chem. 1995, 270, 5950.
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(a) For PAR-2: Nystedt, S., Emilsson, K., Wahlestedt, C., Sundelin, J. Proc. Natl. Acad Sci. U.S.A.1994, 91, 9208. Nystedt, S.; Emilsson, K.; Larsson, A.-K.; Stroembeck, B.; Sundelin, J. Eur. J. Biochem. 1995, 232, 84. Nystedt, S.; Larsson, A.-K.; Aberg, H.; Sundelin, J. J. Biol. Chem. 1995, 270, 5950.
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(a) For PAR-2: Nystedt, S., Emilsson, K., Wahlestedt, C., Sundelin, J. Proc. Natl. Acad Sci. U.S.A.1994, 91, 9208. Nystedt, S.; Emilsson, K.; Larsson, A.-K.; Stroembeck, B.; Sundelin, J. Eur. J. Biochem. 1995, 232, 84. Nystedt, S.; Larsson, A.-K.; Aberg, H.; Sundelin, J. J. Biol. Chem. 1995, 270, 5950.
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(b) For PAR-3: Ishihara, H.; Connolly, A, J.; Zeng, D.; Kahn, M. L.; Zheng, Y. W.; Timmons, C.; Tram, T.; Coughlin, S. R. Nature 1997, 386, 502.
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(c) For PAR-4: Xu, W.-F.; Andersen, H.; Whitmore, T. E.; Presnell, S. R.; Yee, D. P.; Ching, A.; Gilbert, T.; Davie, E. W.; Foster, D. C. Proc. Natl. Acad. Sci. U.S.A. 1998, 95, 6642. Kahn, M. L.; Zheng, Y.-W.; Huang, W.; Bigornia, V.; Zeng, D.; Moff, S.; Farese, R. V., Jr.; Tam, C.; Coughlin, S. R. Nature 1998, 394, 690.
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Ching, A.6
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Foster, D.C.9
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(c) For PAR-4: Xu, W.-F.; Andersen, H.; Whitmore, T. E.; Presnell, S. R.; Yee, D. P.; Ching, A.; Gilbert, T.; Davie, E. W.; Foster, D. C. Proc. Natl. Acad. Sci. U.S.A. 1998, 95, 6642. Kahn, M. L.; Zheng, Y.-W.; Huang, W.; Bigornia, V.; Zeng, D.; Moff, S.; Farese, R. V., Jr.; Tam, C.; Coughlin, S. R. Nature 1998, 394, 690.
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(a) Feng, D.-M.; Veber, D. F.; Connolly, T. M.; Condra, C.; Tang, M.-J.; Nutt, R. F. J. Med. Chem. 1995, 38, 4125.
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We have reported antagonists of PAR-1 containing a heterocyclic template, see: Hoekstra, W. J.; Hulshizer, B. L.; McComsey, D. F.; Andrade-Gordon, P.; Kauffman, J. A.; Addo, M. F.; Oksenberg, D.; Scarborough, R. M; Maryanoff, B. E. Bioorg. Med. Chem. Lett. 1998, 8, 649.
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24
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(b) Atherton, E.; Logan, C. J.; Sheppard, R. C. J. Chem. Soc., Perkin Trans, 1 1981, 538.
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26
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0013478642
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note
-
1H NMR; they were >90% pure by NMR. Seven compounds besides 4 were purified by HPLC (see Table).
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27
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0030591845
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Greco, M. N.; Powell, E. T.; Hecker, L. R.; Andrade-Gordon, P.; Kauffman, J. A.; Lewis, J. M.; Ganesh, V.; Tulinsky, A.; Maryanoff, B. E. Bioorg. Med. Chem. Lett. 1996, 6, 2947.
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Maryanoff, B.E.9
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28
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0029031716
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Hoekstra, W. J.; Beavers, M. P.; Andrade-Gordon, P.; Evangelisto, M. E.; Keane, P. M.; Press, J. B.; Tomko, K. A.; Fan, F.; Kloczewiak, M.; Mayo, K. H.; Durkin, K. A.; Liotta, D. C. J. Med. Chem. 1995, 38, 1582.
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Press, J.B.6
Tomko, K.A.7
Fan, F.8
Kloczewiak, M.9
Mayo, K.H.10
Durkin, K.A.11
Liotta, D.C.12
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29
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0029758276
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Bernatowitz, M. S.; Klimas, C. E.; Hartl, K. S.; Peluso, M.; Allegretto, N. J.; Seiler, S. M. J. Med. Chem. 1996, 39, 4879.
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30
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0013478059
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Inhibition of human platelet aggregation induced by human α-thrombin (see ref 13)
-
Inhibition of human platelet aggregation induced by human α-thrombin (see ref 13).
-
-
-
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31
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0013552608
-
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note
-
Abbreviations not defined earlier in this paper: Fmoc = 9-fluorenylmethoxycarbonyl; BOP-Cl = N,N'- bis(2-oxo-3-oxazolidinyl)phosphinyl chloride; DMAP = 4-(dimethylamino)pyridine; TFA = trifluoroacetic acid; PMC = 2,2,5,7,8-pentamethylchroman-6-sulfonyl; Har = homoarginine.
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