1.
Bioorg Med Chem Lett
; 16(16): 4252-6, 2006 Aug 15.
Article
in English
| MEDLINE
| ID: mdl-16759857
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.
Subject(s)
Chemistry, Pharmaceutical/methods , Nerve Tissue Proteins/antagonists & inhibitors , Protein Tyrosine Phosphatases/antagonists & inhibitors , Crystallography, X-Ray , Drug Design , Hydrogen Bonding , Hydrolysis , Models, Chemical , Models, Molecular , Molecular Structure , Receptor-Like Protein Tyrosine Phosphatases, Class 5 , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 16(6): 1574-8, 2006 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-16386905
ABSTRACT
High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.
