Synthesis, Structure–Activity Relationship and Docking Studies of Substituted Aryl Thiazolyl Phenylsulfonamides as Potential Protein Tyrosine Phosphatase 1B Inhibitors

Abstract

28 to 1—not bad odds: Protein tyrosine phosphatase 1B (PTP1B) is a promising target for the treatment of type 2 diabetes. Aryl thiazolyl phenylsulfonamides were synthesized and screened against PTP1B in vitro. Compounds exhibiting >48 % inhibition were then evaluated in a streptozotocin-induced (STZ) rat model of diabetes, identifying one compound with efficacy comparable to that of metformin. Finally, docking studies were used to explain the observed structure–activity relationships. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.