Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists

SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described. A series of triazinyl derivatives, such as 4, that block the interaction of VLA-4 integrin with VCAM-1 are described.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-06, Vol.12 (12), p.1591-1594
Hauptverfasser:	Porter, John R., Archibald, Sarah C., Brown, Julien A., Childs, Kirstie, Critchley, David, Head, John C., Hutchinson, Brian, Parton, Ted A.H., Robinson, Martyn K., Shock, Anthony, Warrellow, Graham J., Zomaya, Alex
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Integrin alpha4beta1 - antagonists & inhibitors Medical sciences Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - chemistry Phenylalanine - pharmacology Structure-Activity Relationship Triazines - chemistry Triazines - pharmacology
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Beschreibung
Zusammenfassung:	SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described. A series of triazinyl derivatives, such as 4, that block the interaction of VLA-4 integrin with VCAM-1 are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00237-8