Bioorganic & medicinal chemistry letters, 2004-03, Vol.14 (5), p.1229-1234
2004
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Details
- Autor(en) / Beteiligte
- Titel
- 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor xa inhibitors. Part 3: Design, synthesis and sar of orally bioavailable benzamidine-P4 inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2004-03, Vol.14 (5), p.1229-1234
- Ort / Verlag
- Oxford: Elsevier
- Erscheinungsjahr
- 2004
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro anticoagulant activity. These benzamidine-P4 fXa inhibitors have displayed excellent oral bioavailability and long half-life.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2003.12.054Titel-ID: cdi_proquest_miscellaneous_80179013
- Format
- –
- Schlagworte
- Administration, Oral, Amides - administration & dosage, Amides - chemical synthesis, Amides - metabolism, Animals, Antithrombin III - administration & dosage, Antithrombin III - chemical synthesis, Antithrombin III - metabolism, Benzamidines - antagonists & inhibitors, Benzamidines - metabolism, Biological and medical sciences, Biological Availability, Blood. Blood coagulation. Reticuloendothelial system, Drug Design, Humans, Medical sciences, Pharmacology. Drug treatments, Pyrazoles - administration & dosage, Pyrazoles - chemical synthesis, Pyrazoles - metabolism, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship