Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold

Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the beta-alanine 3-substituent produced compounds that are potent and selective alpha(v)beta(3) antagonists and exhibit a range of physicochemical...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-05, Vol.13 (10), p.1809
Main Authors: Breslin, Michael J, Duggan, Mark E, Halczenko, Wasyl, Fernandez-Metzler, Carmen, Hunt, Cecilia A, Leu, Chih-Tai, Merkle, Kara M, Naylor-Olsen, Adel M, Prueksaritanont, Thomayant, Stump, Gary, Wallace, Audrey, Rodan, Sevgi B, Hutchinson, John H
Format: Article
Language:English
Subjects:
Alanine - chemistry
Drug Design
Humans
Hydrophobic and Hydrophilic Interactions
Inhibitory Concentration 50
Integrin alphaVbeta3 - antagonists & inhibitors
Molecular Mimicry
Oligopeptides
Protein Binding
Pyrazines - chemistry
Pyrazines - pharmacokinetics
Pyridones - chemistry
Pyridones - pharmacokinetics
Radioimmunoassay
Structure-Activity Relationship
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Summary:Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the beta-alanine 3-substituent produced compounds that are potent and selective alpha(v)beta(3) antagonists and exhibit a range of physicochemical properties.
ISSN:0960-894X