2ei6

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{{STRUCTURE_2ei6| PDB=2ei6 | SCENE= }}
{{STRUCTURE_2ei6| PDB=2ei6 | SCENE= }}
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'''FACTOR XA IN COMPLEX WITH THE INHIBITOR (-)-cis-N1-[(5-Chloroindol-2-yl)carbonyl]-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine'''
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===FACTOR XA IN COMPLEX WITH THE INHIBITOR (-)-cis-N1-[(5-Chloroindol-2-yl)carbonyl]-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine===
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==Overview==
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This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane derivative 3j had potent anticoagulant activity as well as anti-fXa activity. Synthetic study of the optical isomers of 3g demonstrated that (-)-3g had more potent activity.
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The line below this paragraph, {{ABSTRACT_PUBMED_17555959}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17555959 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17555959}}
==About this Structure==
==About this Structure==
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[[Category: Protein inhibitor complex]]
[[Category: Protein inhibitor complex]]
[[Category: Serine protease]]
[[Category: Serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 02:35:16 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 20:23:26 2008''

Revision as of 17:23, 28 July 2008

Template:STRUCTURE 2ei6

FACTOR XA IN COMPLEX WITH THE INHIBITOR (-)-cis-N1-[(5-Chloroindol-2-yl)carbonyl]-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine

Template:ABSTRACT PUBMED 17555959

About this Structure

2EI6 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors., Nagata T, Yoshino T, Haginoya N, Yoshikawa K, Isobe Y, Furugohri T, Kanno H, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4683-8. Epub 2007 May 25. PMID:17555959

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