Article ; Online: Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
Bioorganic & medicinal chemistry letters
2007 Volume 17, Issue 24, Page(s) 6910–6913
Abstract: ... synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent ... Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were ...
Abstract | Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats. |
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MeSH term(s) | Anticoagulants/chemical synthesis ; Anticoagulants/chemistry ; Anticoagulants/pharmacology ; Antithrombin III/chemical synthesis ; Antithrombin III/chemistry ; Antithrombin III/pharmacology ; Crystallography, X-Ray ; Factor Xa/chemistry ; Factor Xa/metabolism ; Glycine/analogs & derivatives ; Glycine/chemical synthesis ; Glycine/chemistry ; Glycine/pharmacology ; Humans ; Models, Molecular ; Molecular Structure ; Protein Binding ; Structure-Activity Relationship |
Chemical Substances | Anticoagulants ; phenylglycinamide ; Antithrombin III (9000-94-6) ; Factor Xa (EC 3.4.21.6) ; Glycine (TE7660XO1C) |
Language | English |
Publishing date | 2007-12-15 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 1063195-1 |
ISSN | 1464-3405 ; 0960-894X |
ISSN (online) | 1464-3405 |
ISSN | 0960-894X |
DOI | 10.1016/j.bmcl.2007.09.105 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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