Bioorganic & medicinal chemistry letters, 2001-10, Vol.11 (19), p.2619-2622
2001
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Details
- Autor(en) / Beteiligte
- Titel
- 1,2,4-Triazolo[3,4- a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2001-10, Vol.11 (19), p.2619-2622
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2001
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- Conformationally constrained analogues of the GPIIb/IIIa antagonist elarofiban (RWJ-53308) have been synthesized and biologically evaluated. The 1,2,4-triazolo[3,4- a]pyridine scaffold provided potent antagonists with favorable pharmacodynamic and pharmacokinetic attributes in dogs. Compounds 12a and 13a exhibited enhancements in oral bioavailability, t 1/2, and ex vivo duration of action (inhibition of ADP-induced platelet aggregation) relative to elarofiban. Conformationally constrained triazolopyridine analogues of elarofiban were prepared, leading to compounds with improved pharmacodynamic and pharmacokinetic properties.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(01)00529-7Titel-ID: cdi_proquest_miscellaneous_71166478
- Format
- –
- Schlagworte
- Animals, Biological and medical sciences, Blood. Blood coagulation. Reticuloendothelial system, Dogs, Medical sciences, Nipecotic Acids - chemical synthesis, Nipecotic Acids - chemistry, Nipecotic Acids - pharmacokinetics, Nipecotic Acids - pharmacology, Pharmacology. Drug treatments, Platelet Aggregation Inhibitors - chemical synthesis, Platelet Aggregation Inhibitors - chemistry, Platelet Aggregation Inhibitors - pharmacokinetics, Platelet Aggregation Inhibitors - pharmacology, Platelet Glycoprotein GPIIb-IIIa Complex - antagonists & inhibitors, Pyridines - chemical synthesis, Pyridines - chemistry, Pyridines - pharmacokinetics, Pyridines - pharmacology, Triazoles - chemistry