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1mu8

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[[Image:1mu8.jpg|left|200px]]
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{{STRUCTURE_1mu8| PDB=1mu8 | SCENE= }}
{{STRUCTURE_1mu8| PDB=1mu8 | SCENE= }}
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'''thrombin-hirugen_l-378,650'''
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===thrombin-hirugen_l-378,650===
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==Overview==
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Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2-phenethylamino)-6-methylpyrazinone acetamide template (e.g., 1) which resulted in the modification of each of the three principal components (i.e., P1, P2, P3) comprising this series. As a result of these studies, several potent thrombin inhibitors (e.g., 20, 24, 25) were identified which exhibit high levels of oral bioavailability and long plasma half-lives.
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{{ABSTRACT_PUBMED_12570369}}
==About this Structure==
==About this Structure==
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[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
[[Category: Thrombin-hirugen]]
[[Category: Thrombin-hirugen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:39:21 2008''

Revision as of 03:39, 29 July 2008

Image:1mu8.png

Template:STRUCTURE 1mu8

thrombin-hirugen_l-378,650

Template:ABSTRACT PUBMED 12570369

About this Structure

1MU8 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines., Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, J Med Chem. 2003 Feb 13;46(4):461-73. PMID:12570369

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