title: 5,6-Diarylanthranilo-1,3-dinitriles as a new class of antihyperglycemic agents.
abstract: Various functionalized mono- and diarylanthranilo-1,3-dinitriles were synthesized and evaluated for their in vitro antihyperglycemic activity against the PTP-1B, glucose-6-phosphatase, glycogen phosphorylase and alpha-glucosidase enzymes. Among various screened compounds, 5,6-diaryl substituted anthranilo-1,3-dinitriles 3a, 3b, and 3d showed good inhibitory activity against PTP-1B with IC(50) values of 58-72 microM. Three of the test compounds showed significant (25-37%) lowering of plasma glucose level at 24h in sucrose-challenged streptozotocin-induced diabetic Sprague-Dawley rat model.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India.
authors.forename: Fateh V
authors.initials: FV
authors.lastname: Singh
authors.forename: Amrita
authors.initials: A
authors.lastname: Parihar
authors.forename: Sumit
authors.initials: S
authors.lastname: Chaurasia
authors.forename: Amar B
authors.initials: AB
authors.lastname: Singh
authors.forename: Salil P
authors.initials: SP
authors.lastname: Singh
authors.forename: Akhilesh K
authors.initials: AK
authors.lastname: Tamrakar
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: Atul
authors.initials: A
authors.lastname: Goel
mesh_terms: D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000145:classification* / Q000627:therapeutic use; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D007004:Hypoglycemic Agents