2fes

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[[Image:2fes.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2fes| PDB=2fes | SCENE= }}
{{STRUCTURE_2fes| PDB=2fes | SCENE= }}
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'''Orally active thrombin inhibitors'''
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===Orally active thrombin inhibitors===
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==Overview==
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The synthesis and SAR of novel nanomolar thrombin inhibitors with the common backbone HOOC-CH(2)-d-cyclohexylalanyl-3,4-dehydroprolyl-NH-CH(2)-aryl-C(=NH)NH(2) are described together with their ecarin clotting time (ECT) prolongation as measure for thrombin inhibition ex vivo. The aryl P1-moiety mimicking the arginine part of the d-Phe-Pro-Arg derived thrombin inhibitors turned out to be a key component for in vitro potency and in vivo activity. Optimization of this part led to compounds with improved antithrombin activity in rats and dogs after oral administration compared to the recently launched anticoagulant melagatran.
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The line below this paragraph, {{ABSTRACT_PUBMED_16517159}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16517159 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16517159}}
==About this Structure==
==About this Structure==
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[[Category: Hoeffken, H W.]]
[[Category: Hoeffken, H W.]]
[[Category: Thrombin inhibitor]]
[[Category: Thrombin inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:48:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:14:03 2008''

Revision as of 10:14, 29 July 2008

Image:2fes.png

Template:STRUCTURE 2fes

Orally active thrombin inhibitors

Template:ABSTRACT PUBMED 16517159

About this Structure

2FES is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety., Mack H, Baucke D, Hornberger W, Lange UE, Seitz W, Hoffken HW, Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6. PMID:16517159

Page seeded by OCA on Tue Jul 29 13:14:03 2008

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