title: Synthesis of functionalized acetophenones as protein tyrosine phosphatase 1B inhibitors.
abstract: Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP1B knock-out mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of functionalized acetophenones were synthesized and evaluated for their PTP1B inhibitory activity. Some of the screened compounds displayed good inhibitory activity.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Manish
authors.initials: M
authors.lastname: Dixit
authors.forename: Brajendra K
authors.initials: BK
authors.lastname: Tripathi
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: Atul
authors.initials: A
authors.lastname: Goel
mesh_terms: D000098:Acetophenones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000098:Acetophenones; D004791:Enzyme Inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases