QSAR Studies on A Series of N2-Aryltriazolinone Biphenylsulfonamide Derivatives in Order to Evolve Potent and Orally Active Angiotensin II Receptor Antagonists

 

Preeti Tiwari* and J. P. Mishra

Department of Chemistry, F.G. College, Rae Bareli - 229 001 (India).

Quantitative structure activity relationship (QSAR) studies have been performed on a series of N2 – Aryltriazolinone Biphenyl sulfonamide derivatives, using physico-chemical parameters such as hydrophobicity (p), molar refractivity (MR), field effect (F) resonance effect (R) and electronic properties. Binding affinities of these derivatives for the AT1 and AT2 receptor subtype of angiotensin II in human adrenal assays was found to have strong correlation with hydrophobicity (p) of the substituent at R1 position and molar refractivity of the substituent at R3 position. The presence of F atom at X position was also found to be important for activity.

QSAR; aryltriazolinone; antagonists