N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists.
The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described.
Porter
John R
JR
Celltech R&D Ltd, 216 Bath Road, SL1 4EN, Slough, 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*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D039041:Integrin alpha4beta1; C468809:N-(pyridin-2-yl) phenylalanine; C468810:N-(pyrimidin-4-yl) phenylalanine; D011725:Pyridines; D011743:Pyrimidines; D010649:Phenylalanine