N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists

John R Porter; Sarah C Archibald; Julien A Brown; Kirstie Childs; David Critchley; John C Head; Brian Hutchinson; Ted A H Parton; Martyn K Robinson; Anthony Shock; Graham J Warrellow; Alex Zomaya

doi:10.1016/s0960-894x(02)00241-x

N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1595-8. doi: 10.1016/s0960-894x(02)00241-x.

Authors

John R Porter¹, Sarah C Archibald, Julien A Brown, Kirstie Childs, David Critchley, John C Head, Brian Hutchinson, Ted A H Parton, Martyn K Robinson, Anthony Shock, Graham J Warrellow, Alex Zomaya

Affiliation

¹ Celltech R&D Ltd, 216 Bath Road, SL1 4EN, Slough, UK. john.porter@celltechgroup.com

PMID: 12039570
DOI: 10.1016/s0960-894x(02)00241-x

Abstract

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.

MeSH terms

Integrin alpha4beta1 / antagonists & inhibitors*
Phenylalanine / analogs & derivatives
Phenylalanine / chemistry*
Phenylalanine / pharmacology*
Pyridines / chemistry*
Pyridines / pharmacology*
Pyrimidines / chemistry*
Pyrimidines / pharmacology*
Structure-Activity Relationship

Substances

Integrin alpha4beta1
N-(pyridin-2-yl) phenylalanine
N-(pyrimidin-4-yl) phenylalanine
Pyridines
Pyrimidines
Phenylalanine