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D'Amico, D. C.; Aya, T.; Human, J.; Fotsch, C.; Chen, J. J.; Biswas, K.; Riahi, B.; Norman, M. H.; Willoughby, C. A.; Hungate, R.; Reider, P. J.; Biddlecome, G.; Lester-Ziener, D.; Van Staden, C.; Johnson, E.; Kamassah, A.; Arik, L.; Wang, J.; Viswanadhan, V. N.; Groneberg, R. D.; Zhan, J.; Suzuki, H.; Toro, A.; Mareska, D. A.; Clarke, D. E.; Harvey, D. M.; Burgess, L. E.; Laird, E. R.; Askew, B.; Ng, G. Identification of a Nonpeptidic and Conformationally Restricted Bradykinin 1 Antagonist with Anti-Inflammatory Activity. J. Med. Chem. 2007, 50, 607-610.
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D'Amico, D. C.; Aya, T.; Human, J.; Fotsch, C.; Chen, J. J.; Biswas, K.; Riahi, B.; Norman, M. H.; Willoughby, C. A.; Hungate, R.; Reider, P. J.; Biddlecome, G.; Lester-Ziener, D.; Van Staden, C.; Johnson, E.; Kamassah, A.; Arik, L.; Wang, J.; Viswanadhan, V. N.; Groneberg, R. D.; Zhan, J.; Suzuki, H.; Toro, A.; Mareska, D. A.; Clarke, D. E.; Harvey, D. M.; Burgess, L. E.; Laird, E. R.; Askew, B.; Ng, G. Identification of a Nonpeptidic and Conformationally Restricted Bradykinin 1 Antagonist with Anti-Inflammatory Activity. J. Med. Chem. 2007, 50, 607-610.
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34247626591
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Compound 2 and all analogues reported herein possess two benzylic amines: one present as an amide and the other as an amine. For purposes of clarification, the amine is marked with an asterisk in Figure 1 and is referred to as the benzylic amine throughout the text.
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Compound 2 and all analogues reported herein possess two benzylic amines: one present as an amide and the other as an amine. For purposes of clarification, the amine is marked with an asterisk in Figure 1 and is referred to as the "benzylic amine" throughout the text.
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There were other potent piperidine replacements identified as part of the SAR study in Table 1 (e.g., the 1-morpholino analog 17), but those compounds suffered from poor pharmacokinetic properties (data not shown) and are not discussed further in this study.
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There were other potent piperidine replacements identified as part of the SAR study in Table 1 (e.g., the 1-morpholino analog 17), but those compounds suffered from poor pharmacokinetic properties (data not shown) and are not discussed further in this study.
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