title: Squaric acid derivatives as VLA-4 integrin antagonists.
abstract: SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.
authors.affiliation: Celltech R&D Ltd, 216 Bath Road, Slough SL1 4EN, UK. john.porter@celltechgroup.com
authors.forename: John R
authors.initials: JR
authors.lastname: Porter
authors.forename: Sarah C
authors.initials: SC
authors.lastname: Archibald
authors.forename: Kirstie
authors.initials: K
authors.lastname: Childs
authors.forename: David
authors.initials: D
authors.lastname: Critchley
authors.forename: John C
authors.initials: JC
authors.lastname: Head
authors.forename: Janeen M
authors.initials: JM
authors.lastname: Linsley
authors.forename: Ted A H
authors.initials: TA
authors.lastname: Parton
authors.forename: Martyn K
authors.initials: MK
authors.lastname: Robinson
authors.forename: Anthony
authors.initials: A
authors.lastname: Shock
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Taylor
authors.forename: Graham J
authors.initials: GJ
authors.lastname: Warrellow
authors.forename: Rikki P
authors.initials: RP
authors.lastname: Alexander
authors.forename: Barry
authors.initials: B
authors.lastname: Langham
mesh_terms: D000588:Amines / Q000737:chemistry; D000818:Animals; D018926:Anti-Allergic Agents / Q000037:antagonists & inhibitors*; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D039041:Integrin alpha4beta1; D019012:Integrin beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D008657:Metabolic Clearance Rate; D051381:Rats; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D016029:Receptors, Very Late Antigen; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D018926:Anti-Allergic Agents; D003503:Cyclobutanes; D039041:Integrin alpha4beta1; D019012:Integrin beta1; D016023:Integrins; D016201:Receptors, Lymphocyte Homing; D016029:Receptors, Very Late Antigen; C030042:squaric acid