Imidazopyridines as VLA-4 integrin antagonists.
We describe a novel series of imidazopyridine substituted phenylalanines which are potent VLA-4 antagonists. A wide variety of substituents are tolerated as replacements for the pendant 3-pyridyl ring. A clear structure-activity relationship was identified around the substitution of the 3-amino-cyclobut-2-enone portion of the molecule.
UCB, Granta Park, Great Abington, Cambridge CB21 6GS, UK. david.phillips@ucb-group.com
David J
DJ
Phillips
Richard J
RJ
Davenport
Thierry A
TA
Demaude
Fiona P
FP
Galleway
Mark W
MW
Jones
Laurent
L
Knerr
Benjamin G
BG
Perry
Andrew J
AJ
Ratcliffe
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors* / Q000097:blood; D051379:Mice; D008956:Models, Chemical; D008968:Molecular Conformation; D010649:Phenylalanine / Q000737:chemistry*; D011485:Protein Binding; D011725:Pyridines / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship
D039041:Integrin alpha4beta1; D011725:Pyridines; D010649:Phenylalanine