Bioorganic & medicinal chemistry letters, 2003-03, Vol.13 (6), p.1067-1070
2003
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Details
- Autor(en) / Beteiligte
- Titel
- The identification of clinical candidate SB-480848 : A potent inhibitor of lipoprotein-associated phospholipase A2
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2003-03, Vol.13 (6), p.1067-1070
- Ort / Verlag
- Oxford: Elsevier
- Erscheinungsjahr
- 2003
- Quelle
- ScienceDirect
- Beschreibungen/Notizen
- Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency. Cyclopentyl fused derivative 21, SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(03)00058-1Titel-ID: cdi_proquest_miscellaneous_73108456
- Format
- –
- Schlagworte
- 1-Alkyl-2-acetylglycerophosphocholine Esterase, Animals, Biological and medical sciences, Cytochrome P-450 CYP2D6 Inhibitors, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, General and cellular metabolism. Vitamins, Humans, In Vitro Techniques, Kinetics, Medical sciences, Pharmacology. Drug treatments, Phospholipases A - antagonists & inhibitors, Phospholipases A - blood, Phospholipases A2, Pyrimidinones - chemistry, Pyrimidinones - pharmacology, Rabbits, Recombinant Proteins - antagonists & inhibitors