title: Synthesis of protein tyrosine phosphatase 1B inhibitors: model validation and docking studies.
abstract: The designed and synthesized 2-(4-methoxyphenyl) ethyl] acetamide derivatives (3a, 3b and 3c) were evaluated for their PTP1B inhibitory activity where they showed IC(50) values 69 microM, 87 microM and 71 microM, respectively. These results correlated well with the docking studies and in vivo screening of the compounds for their antidiabetic activity in SLM and STZ models.
authors.affiliation: Central Drug Research Institute, Medicinal and Process Chemistry, Chattar Manzil Palace, Mahatma Gandhi Marg, Lucknow, Uttar Pradesh, India. anilsak@gmail.com
authors.forename: Anil K
authors.initials: AK
authors.lastname: Saxena
authors.forename: Gyanendra
authors.initials: G
authors.lastname: Pandey
authors.forename: Swati
authors.initials: S
authors.lastname: Gupta
authors.forename: Amar Bahadur
authors.initials: AB
authors.lastname: Singh
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
mesh_terms: D000818:Animals; D001665:Binding Sites / Q000502:physiology; D018360:Crystallography, X-Ray; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy* / Q000201:enzymology; D016503:Drug Delivery Systems / Q000379:methods*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D008958:Models, Molecular; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism; D051381:Rats
chemical_list: D007004:Hypoglycemic Agents; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1