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.
Porter
John R
JR
Celltech R&D Ltd, 216 Bath Road, Slough SL1 4EN, UK. john.porter@celltechgroup.com
Archibald
Sarah C
SC
Brown
Julien A
JA
Childs
Kirstie
K
Critchley
David
D
Head
John C
JC
Hutchinson
Brian
B
Parton
Ted A H
TA
Robinson
Martyn K
MK
Shock
Anthony
A
Warrellow
Graham J
GJ
Zomaya
Alex
A
D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors*; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry* / Q000494:pharmacology*
D039041:Integrin alpha4beta1; C468808:N-(triazin-1,3,5-yl) phenylalanine; D014227:Triazines; D010649:Phenylalanine