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The effect of fluorine substitution on the physicochemical properties and the analgesic activity of paracetamol

S BARNARD, RC Storr, PM O'NEILL…

文献索引:Barnard; Storr; O'Neill; Park Journal of Pharmacy and Pharmacology, 1993 , vol. 45, # 8 p. 736 - 744

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被引用次数: 19

摘要

Abstract—The physicochemical properties and analgesic action of six fluorinated analogues of 4-hydroxyacetanilide (paracetamol) have been investigated. Fluorine substitution adjacent to the hydroxyl group increased lipophilicity and oxidation potential whilst substitution adjacent to the amide had little effect on lipophilicity but led to a greater increase in oxidation potential. Lack of coplanarity and conjugation of the amide group and ...