Inhibitors of Adenosine 3', 5'-Cyclic Monophosphate Phosphodiesterase from Schisandra chinensis and the Structure Activity Relationship of Lignans

概要

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The structure activity relationship was studied in analogous lignans from Schisandra chinensis and their derivatives. These compounds were tested for cyclic adenosine 3', 5'-monophosphate (cAMP) phosphodiesterase inhibition. An inhibitor, nordihydroguaiaretic acid (13), was isolated from this plant, so we discussed this compound and a derivative, nordihydroguaiaretic acid tetramethyl ether, using molecular mechanics involving three-dimensional modeling and minimization of the structure using the MM2PP program. As a result, it was found that the structure of nordihydroguaiaretic acid tetrametyl ether and papaverine (30) (positive control) shared a similar low energy conformation. This fact suggested that these compounds inhibited cAMP phosphodiesterase by a similar mechanism.
社団法人日本薬学会の論文
1992-05-25