QSAR Optimization of Benzofuran and Benzothiophene Sulfono Biphenyl as Potent PTPase-1B Inhibitors

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Title QSAR Optimization of Benzofuran and Benzothiophene Sulfono Biphenyl as Potent PTPase-1B Inhibitors
 
Creator Darpan Kaushik; F/O Pharmacy, Jamia Hamdard University, New Delhi-110062, India
Suroor A Khan; F/O Pharmacy, Jamia Hamdard University, New Delhi-110062, India
Ozair Alam; F/O Pharmacy, Jamia Hamdard University, New Delhi-110062, India
Geeta Chawla; F/O Pharmacy, Jamia Hamdard University, New Delhi-110062, India
Satish G Kashedikar; Shri G.S. Institute of Technology and Sciences, Indore-452003, M.P., India
 
Subject Pharmacology
QSAR; PTPase-1B inhibitor; Sulfono biphenyl analog
 
Description Insulin resistance is associated with a defect in protein tyrosine phosphorylation in the insulin signal transduction cascade. Protein tyrosine phosphatase (PTPase) enzyme dephosphorylates the active form of insulin receptor and thus attenuates its tyrosine kinase activity, therefore the need of potent PTPase inhibitor is there with that intention the Quantitative structure-activity relationship QSAR was performed. QSAR has been established on a series of compounds of novel sulfono biphenyl analogs using SYSTAT (Version 7.0) software, for their PTPase-1B inhibitor activity, in order to understand the essential structural requirement for binding with the receptor. Among several 2D QSAR models, one for a series was selected on the basis of high correlation coefficient, least standard deviation, & high value of significance for maximum no. of subject was considered. The interpreted data signify the essentiality of Benzofuran ring in the designing of the new PTPase -1B inhibitors and any substitution on the biphenyl and sulfonyl phenyl is going to decrease its activity. Key words: QSAR, PTPase-1B inhibitor, Sulfono biphenyl analog. Dhaka Univ. J. Pharm. Sci. 6(2): 77-80, 2007 (December)
 
Publisher Dhaka University
 
Date 2008-02-15
 
Type
 
Format application/pdf
 
Identifier http://www.banglajol.info/index.php/JPharma/article/view/679
 
Source Dhaka University Journal of Pharmaceutical Sciences; Vol 6, No 2 (2007); 77-80
 
Language en
 
Coverage Bangladesh