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Abstract

Quantitative structure - activity relationship study of antihistaminic thiazolidin-4-ones.

Author(s): P Singh, TN Ojha, RC Sharma, S Tiwari
Dept. of Chemistry S.K. Government College, Sikar - 332001

Correspondence Address:
P Singh Dept. of Chemistry S.K. Government College, Sikar - 332001

The quantitative structure-activity relationship (QSAR) studies of some substituted thiazolidin-4-ones have yielded statistically sound correlation between the observed potency of histamine antagonism, pA2, which in turn is nearly linearly correlated with the inhibitory activity,-logIC50 and physicochemical parameters such as the overall field effect,F, and hydrophobic effect at the 4-position,pi4, generated by R-substituents in the phenyl ring. In the light of our present findings a compound with pA2 approaching 2 orders of magnitude greater than that of the most active compound of the parent series is predicted.