QSAR studies on a series of N-2-aryltriazolinone biphenylsulfonamide derivatives in order to evolve potent and orally active angiotensin II receptor antagonists

Quantitative structure activity relationship (QSAR) studies have been performed on a series of N-2 - Aryltriazolinone Biphenyl sulfonamide derivatives, using physico-chemical parameters such as hydrophobicity (pi), molar refractivity (MR), field effect (F) resonance effect (R) and electronic properties. Binding affinities of these derivatives for the AT(1) and AT(2) receptor subtype of angiotensin II in human adrenal assays was found to have strong correlation with hydrophobicity (p) of the substituent at R-1 position and molar refractivity of the substituent at R-3 position. The presence of F atom at X position was also found to be important for activity.