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1z6e

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[[Image:1z6e.gif|left|200px]]
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{{STRUCTURE_1z6e| PDB=1z6e | SCENE= }}
{{STRUCTURE_1z6e| PDB=1z6e | SCENE= }}
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'''Crystal Structure of Factor Xa complexed to Razaxaban'''
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===Crystal Structure of Factor Xa complexed to Razaxaban===
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==Overview==
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Modification of a series of pyrazole factor Xa inhibitors to incorporate an aminobenzisoxazole as the P(1) ligand resulted in compounds with improved selectivity for factor Xa relative to trypsin and plasma kallikrein. Further optimization of the P(4) moiety led to compounds with enhanced permeability and reduced protein binding. The SAR and pharmacokinetic profile of this series of compounds is described herein. These efforts culminated in 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimeth ylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide (11d), a potent, selective, and orally bioavailable inhibitor of factor Xa. On the basis of its excellent in vitro potency and selectivity profile, high free fraction in human plasma, good oral bioavailability, and in vivo efficacy in antithrombotic models, the HCl salt of this compound was selected for clinical development as razaxaban (DPC 906, BMS-561389).
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(as it appears on PubMed at http://www.pubmed.gov), where 15771420 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15771420}}
==About this Structure==
==About this Structure==
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[[Category: Coagulation cascade]]
[[Category: Coagulation cascade]]
[[Category: Factor xa]]
[[Category: Factor xa]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:13:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:10:24 2008''

Revision as of 07:10, 28 July 2008

Image:1z6e.png

Template:STRUCTURE 1z6e

Crystal Structure of Factor Xa complexed to Razaxaban

Template:ABSTRACT PUBMED 15771420

About this Structure

1Z6E is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor., Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR, J Med Chem. 2005 Mar 24;48(6):1729-44. PMID:15771420

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