2phb

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{{STRUCTURE_2phb| PDB=2phb | SCENE= }}
{{STRUCTURE_2phb| PDB=2phb | SCENE= }}
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'''An Orally Efficacious Factor Xa Inhibitor'''
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===An Orally Efficacious Factor Xa Inhibitor===
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==Overview==
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Herein, we report the discovery of novel, proline-based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional incorporation of 1-(4-amino-3-fluoro-phenyl)-1H-pyridin-2-one 22, as a P4 pharmacophore, we discovered compound 7 (PD 0348292). This compound is a selective, orally bioavailable, efficacious FXa inhibitor that is currently in phase II clinical trials for the treatment and prevention of thrombotic disorders.
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(as it appears on PubMed at http://www.pubmed.gov), where 17683371 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17683371}}
==Disease==
==Disease==
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[[Category: Blood clotting]]
[[Category: Blood clotting]]
[[Category: Fxa coagulation factor inhibitor]]
[[Category: Fxa coagulation factor inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 13:06:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 18:48:30 2008''

Revision as of 15:48, 28 July 2008

Image:2phb.png

Template:STRUCTURE 2phb

Contents

An Orally Efficacious Factor Xa Inhibitor

Template:ABSTRACT PUBMED 17683371

Disease

Known disease associated with this structure: Factor X deficiency OMIM:[227600]

About this Structure

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

Reference

The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarb oxamide (PD 0348292), an orally efficacious factor Xa inhibitor., Kohrt JT, Bigge CF, Bryant JW, Casimiro-Garcia A, Chi L, Cody WL, Dahring T, Dudley DA, Filipski KJ, Haarer S, Heemstra R, Janiczek N, Narasimhan L, McClanahan T, Peterson JT, Sahasrabudhe V, Schaum R, Van Huis CA, Welch KM, Zhang E, Leadley RJ, Edmunds JJ, Chem Biol Drug Des. 2007 Aug;70(2):100-12. PMID:17683371

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