title: Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta.
abstract: The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency.
authors.affiliation: Procter & Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040, USA. Amarasinghe.kk@pg.com
authors.forename: Kande K D
authors.initials: KK
authors.lastname: Amarasinghe
authors.forename: Artem G
authors.initials: AG
authors.lastname: Evdokimov
authors.forename: Artem G
authors.initials: AG
authors.lastname: Evidokimov
authors.forename: Kevin
authors.initials: K
authors.lastname: Xu
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Clark
authors.forename: Matthew B
authors.initials: MB
authors.lastname: Maier
authors.forename: Anil
authors.initials: A
authors.lastname: Srivastava
authors.forename: Anny-Odile
authors.initials: AO
authors.lastname: Colson
authors.forename: Gina S
authors.initials: GS
authors.lastname: Gerwe
authors.forename: George E
authors.initials: GE
authors.lastname: Stake
authors.forename: Brian W
authors.initials: BW
authors.lastname: Howard
authors.forename: Matthew E
authors.initials: ME
authors.lastname: Pokross
authors.forename: Jeffrey L
authors.initials: JL
authors.lastname: Gray
authors.forename: Kevin G
authors.initials: KG
authors.lastname: Peters
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray; D015195:Drug Design; D006860:Hydrogen Bonding; D006868:Hydrolysis; D008956:Models, Chemical; D008958:Models, Molecular; D015394:Molecular Structure; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D054633:Receptor-Like Protein Tyrosine Phosphatases, Class 5; D013329:Structure-Activity Relationship
chemical_list: D009419:Nerve Tissue Proteins; D017027:Protein Tyrosine Phosphatases; D054633:Receptor-Like Protein Tyrosine Phosphatases, Class 5