2feq: Difference between revisions

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Bots, Bureaucrats, journal, Administrators
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OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,328,572 edits
No edit summary
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[[Image:2feq.gif|left|200px]]
{{Seed}}
[[Image:2feq.png|left|200px]]


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{{STRUCTURE_2feq|  PDB=2feq  |  SCENE=  }}  
{{STRUCTURE_2feq|  PDB=2feq  |  SCENE=  }}  


'''orally active thrombin inhibitors'''
===orally active thrombin inhibitors===




==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.
The line below this paragraph, {{ABSTRACT_PUBMED_16517159}}, adds the Publication Abstract to the page
(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: Mack, H.]]
[[Category: Mack, H.]]
[[Category: Thrombin inhibitor]]
[[Category: Thrombin inhibitor]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 03:48:37 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:52:29 2008''
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