Optimal Lipophilicity of Sulfonium <i>p</i>-Toluenesulfonate as Anti-allergic Drug

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  • スルホニウム <i>p</i> -トルエンスルホン酸誘導体の抗アレルギー薬としての最適疎水性

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In the development of the anti-allergic drug Suplatast Tosilate (IPD-1151T) we have reported the QSAR analysis using only the calculated π values, because the few logK values of sulfonium compounds had been measured till then. In this study, we measured the logKTLC value of sulfonium compounds by using octylsililated silicagel plate (Merck HPTLC RP-8 F254S). The logKTLC values of the optimized compounds 52 and 67 (Suplatast Tosilate) of dimethylsulfonium p-toluenesulfonates derivatives were 0.07 and 0.06, respectively. Therefore, it was found that the desirable logKTLC value of the sulfonium compound was approximately zero as the anti-allergic drug.

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