title: QSAR studies of benzofuran/benzothiophene biphenyl derivatives as inhibitors of PTPase-1B.
abstract: OBJECTIVE
  Insulin resistance is associated with a defect in protein tyrosine phosphorylation in the insulin signal transduction cascade. The PTPase enzyme dephosphorylates the active form of the insulin receptor and thus attenuates its tyrosine kinase activity, therefore, the need for a potent PTPase inhibitor exists, with the intention of which the QSAR was performed.
  
  
  METHODS
  Quantitative structure-activity relationship (QSAR) has been established on a series of 106 compounds considering 27 variables, for novel biphenyl analogs, using the SYSTAT (Version 7.0) software, for their protein tyrosine phosphatase (PTPase-1B) inhibitor activity, in order to understand the essential structural requirement for binding with the receptor.
  
  
  RESULTS
  Among several regression models, one per series was selected on the basis of a high correlation coefficient (r, 0.86), least standard deviation (s, 0.234), and a high value of significance for the maximum number of subjects (n, 101).
  
  
  CONCLUSIONS
  The influence of the different physicochemical parameters of the substituents in various positions has been discussed by generating the best QSAR model using multiple regression analysis, and the information thus obtained from the present study can be used to design and predict more potent molecules as PTPase-1B inhibitors, prior to their synthesis.
authors.affiliation: F/O Pharmacy, Rajendra Institute of Technology and Sciences, Sirsa-125055, India.
authors.forename: D
authors.initials: D
authors.lastname: Kaushik
authors.forename: R
authors.initials: R
authors.lastname: Kumar
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena