Design and synthesis of potent non-peptidic inhibitors of HPTPβ

Published in: Journal, Article, Volume : 16, Issue : 16, Pages : 4252-4256

DOI : 10.1016/j.bmcl.2006.05.074

Author : Amarasinghe, Kande K. D.; Evidokimov, Artem G.; Xu, Kevin; Clark, Cynthia M.; Maier, Matthew B.; Srivastava, Anil; Colson, Anny-Odile; Gerwe, Gina S.; Stake, George E.; Howard, Brian W.; Pokross, Matthew E.; Gray, Jeffrey L.; Peters, Kevin G.

Abstract : The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPβ. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPβ potency.