title: Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
abstract: A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities towards both CXCR2 and CXCR1 receptors.
authors.affiliation: Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
authors.forename: Cynthia
authors.initials: C
authors.lastname: Aki
authors.forename: Jianping
authors.initials: J
authors.lastname: Chao
authors.forename: Johan A
authors.initials: JA
authors.lastname: Ferreira
authors.forename: Michael P
authors.initials: MP
authors.lastname: Dwyer
authors.forename: Younong
authors.initials: Y
authors.lastname: Yu
authors.forename: Jianhua
authors.initials: J
authors.lastname: Chao
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Merritt
authors.forename: Gaifa
authors.initials: G
authors.lastname: Lai
authors.forename: Minglang
authors.initials: M
authors.lastname: Wu
authors.forename: R William
authors.initials: RW
authors.lastname: Hipkin
authors.forename: Xuedong
authors.initials: X
authors.lastname: Fan
authors.forename: Waldemar
authors.initials: W
authors.lastname: Gonsiorek
authors.forename: James
authors.initials: J
authors.lastname: Fosseta
authors.forename: Diane
authors.initials: D
authors.lastname: Rindgen
authors.forename: Jay
authors.initials: J
authors.lastname: Fine
authors.forename: Daniel
authors.initials: D
authors.lastname: Lundell
authors.forename: Arthur G
authors.initials: AG
authors.lastname: Taveras
authors.forename: Purakkattle
authors.initials: P
authors.lastname: Biju
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000737:chemistry*; D000818:Animals; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000494:pharmacology; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007249:Inflammation; D007700:Kinetics; D008956:Models, Chemical; D019800:Phenol / Q000737:chemistry*; D051381:Rats; D023062:Receptors, Interleukin-8A / Q000037:antagonists & inhibitors*; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D003503:Cyclobutanes; D003959:Diamines; D023062:Receptors, Interleukin-8A; D023063:Receptors, Interleukin-8B; D019800:Phenol