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Asian Journal of Biochemistry

Year: 2006 | Volume: 1 | Issue: 4 | Page No.: 307-315
DOI: 10.3923/ajb.2006.307.315
Quantitative Structure Activity Relationships of Some Selective Inhibitors of Glucagon Receptor: A Hansch Approach
C. Karthikeyan, P. Kumar, N.S. Narayana Moorthy, S.K. Shrivastava and Piyush Trivedi

Abstract: A quantitative structure activity analysis based on linear free energy related approach of Hansch was attempted on a series of glucagon receptor inhibitory triaryl imidazoles. Substituent constants are used to characterize the effect of structural modification on aromatic ring A and B of triaryl imidazole derivatives on glucagon receptor inhibition. The statistically significant correlations deduced by multiple linear regression analysis suggest that steric property of the substituents in aromatic ring B governs the glucagon receptor binding of triaryl imidazoles. The hydrogen acceptor atoms in the aromatic ring B is shown to have a positive influence on the active site binding of triaryl imidazoles whereas the hydrogen acceptor atoms in the aromatic ring A appears to have a negative effect on the inhibitory potency of triaryl imidazoles. Additionally, the study also indicates that bulky substituent in aromatic ring B confers selectivity for glucagon receptor over p38 mitogen activated protein kinase enzyme.

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How to cite this article
C. Karthikeyan, P. Kumar, N.S. Narayana Moorthy, S.K. Shrivastava and Piyush Trivedi, 2006. Quantitative Structure Activity Relationships of Some Selective Inhibitors of Glucagon Receptor: A Hansch Approach. Asian Journal of Biochemistry, 1: 307-315.

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