A quantitative structure—activity relationship analysis of a series of 2′-(2,4-difluorophenoxy)-4′-substituted methanesulfonilides
European Journal of Medicinal Chemistry(1995)
Abstract
A series of antiinflammatory 2′-(2,4-difluorophenoxy)-4′-substituted methanesulfonilides was subjected to quantitative structure—activity relationship (QSAR) analysis. The result of the study showed that the oral antiinflammatory activity, as determined in the rat adjuvant arthritis model, was highly correlated with the electronic (σ1) and steric (Sterimol B1) effects exhibited by the 4′-substitution (R). The relationship can be expressed by the following regression equation: log (% paw edema inhibition) = 1.073(0.304)σ1 + 1.019(0.259)B1 − 2.001(0.411).
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Key words
antiinflammatory activity,structure—,activity relationship,methanesulfonilide
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