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Asian Journal of Biochemistry

Year: 2006 | Volume: 1 | Issue: 4 | Page No.: 307-315
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Authors

C. Karthikeyan

P. Manoj Kumar

N.S. Hari Narayana Moorthy

S.K. Shrivastava

Piyush Trivedi

Keywords

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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