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The optimization of a series of peptidyl thrombin inhibitors utilizing a similar approach was recently described. See
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The optimization of a series of peptidyl thrombin inhibitors utilizing a similar approach was recently described. See: Brady, S. F.; Stauffer, K. J.; Lumma, W. C.; Smith, G. M.; Ramjit, H. G.; Lewis, S. D.; Lucas, B. J.; Gardell, S. J.; Lyle, E. A.; Appleby, S. D.; Cook, J. J.; Holahan, M. A.; Stranieri, M. T.; Lynch, Jr., J. J.; Lin, J. H.; Chen, I.-W.; Vastag, K.; Naylor-Olsen, A. M.; Vacca, J. P. J. Med. Chem. 1998, 41, 401.
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Available Chemicals Directory, v97.1, Molecular Design Limited, 14600 Catalina Street, San Leandro, CA 94577
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Available Chemicals Directory, v97.1, Molecular Design Limited, 14600 Catalina Street, San Leandro, CA 94577.
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0345321361
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Previous structure-activity studies demonstrated that a variety of N-terminal moieties were tolerated in the tripeptide 3CP inhibitor design. See ref. 3b above
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Previous structure-activity studies demonstrated that a variety of N-terminal moieties were tolerated in the tripeptide 3CP inhibitor design. See ref. 3b above.
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24
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0344890182
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Wells containing compounds 8a-g displayed inhibition values ranging from 85% to 97% when tested in the high throughput 3CP enzyme assay system
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Wells containing compounds 8a-g displayed inhibition values ranging from 85% to 97% when tested in the high throughput 3CP enzyme assay system.
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25
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0345321349
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A high-throughput antiviral assay was also utilized to examine compounds 8 prepared on solid phase. However, such examination did not reveal any molecules worthy of solution-phase resynthesis other than those identified by the anti-3CP assay
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A high-throughput antiviral assay was also utilized to examine compounds 8 prepared on solid phase. However, such examination did not reveal any molecules worthy of solution-phase resynthesis other than those identified by the anti-3CP assay.
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26
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0344890163
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The incorporation of additional N-terminal carboxamides derived from aromatic heterocyles into tripeptidyl 3CP inhibitors is ongoing
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The incorporation of additional N-terminal carboxamides derived from aromatic heterocyles into tripeptidyl 3CP inhibitors is ongoing.
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