1mue

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[[Image:1mue.gif|left|200px]]
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{{Seed}}
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[[Image:1mue.png|left|200px]]
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{{STRUCTURE_1mue| PDB=1mue | SCENE= }}
{{STRUCTURE_1mue| PDB=1mue | SCENE= }}
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'''Thrombin-Hirugen-L405,426'''
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===Thrombin-Hirugen-L405,426===
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==Overview==
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In this manuscript we demonstrate that a modification principally directed toward the improvement of the aqueous solubility (i.e., introduction a P3 pyridine N-oxide) of the previous lead compound afforded a new series of potent orally bioavailable P1 N-benzylamide thrombin inhibitors. An expedited investigation of the P1 SAR with respect to oral bioavailability, plasma half-life, and human liver microsome stability revealed 5 as the best candidate for advanced evaluation.
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The line below this paragraph, {{ABSTRACT_PUBMED_12657281}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 12657281 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12657281}}
==About this Structure==
==About this Structure==
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[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
[[Category: Alpha thrombin-hirugen]]
[[Category: Alpha thrombin-hirugen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:43:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:44:31 2008''

Revision as of 03:44, 29 July 2008

Image:1mue.png

Template:STRUCTURE 1mue

Thrombin-Hirugen-L405,426

Template:ABSTRACT PUBMED 12657281

About this Structure

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

Reference

Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides., Burgey CS, Robinson KA, Lyle TA, Nantermet PG, Selnick HG, Isaacs RC, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Stranieri MT, Cook JJ, McMasters DR, Pellicore JM, Pal S, Wallace AA, Clayton FC, Bohn D, Welsh DC, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1353-7. PMID:12657281

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