QSAR IN BRADYKININ ANTAGONISTS - INHIBITION OF THE BRADYKININ-INDUCED CONTRACTION OF THE ISOLATED RAT UTERUS AND GUINEA-PIG ILEUM

Quantitative structure-activity relationships (QSAR) in bradykinin antagonists with activity on rat uterus and/or guinea pig ileum were investigated by the Free-Wilson method in the Fujita-Ban approach. The substituent contributions to antagonist activity were calculated by multiple linear regression. The used QSAR model adequately describes the experimental data, so that the assumption about additivity and independence of the substituent contributions to the overall activity is valid. The obtained results allow a survey of the effect of different modifications on the antagonist potency. Information about the influence of various substitutions on the selectivity of the antagonists can be extracted from the comparison of the QSAR for bath the tissues studied.