Quantitative Structure-Activity Relationships of Ca^<2+>-Antagonistic Semotiadil Congeners

概要

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Structure-Ca^<2+> antagonistic activity relationships of semotiadil (1) congeners having a benzothiazine cyclic system were studied quantitatively by the Hansch-Fujita method. A quadratic dependency of the activity on ClogP, a lipophilic descriptor, of terminal arylalkylamine moieties was suggested. A correlation between the dipole moment component of the 5'-substituted 2-phenylbenzothiazine parts and the potency was also suggested. Additionally, quantitative analysis was successfully shown for the 2-substituted 1 congeners. The results gave information about the mode of binding of 1 with Ca^<2+> receptor.
公益社団法人日本薬学会の論文
1996-03-15