Gobbini M, Marazzi G, Padoani G, Quadri L, Valentino L, Zappavigna M P, Melloni P
Prassis Istituto di Ricerche Sigma-Tau, Settimo Milanese, MI, Italy.
Bioorg Med Chem. 1998 Oct;6(10):1889-94. doi: 10.1016/s0968-0896(98)00119-9.
The four stereoisomers of the 2-hydroxy derivatives of digitoxigenin and 3-epidigitoxigenin have been synthesized, their structures established by NMR, and their binding affinity for the digitalis receptor on Na+, K(+)-ATPase evaluated. These derivatives showed lower affinities than the parent compounds. The hydrophilic hydroxy groups in the alpha position are more detrimental to the affinity than hydroxy groups in the beta position.
洋地黄毒苷元及3-表洋地黄毒苷元的2-羟基衍生物的四种立体异构体已被合成，通过核磁共振确定了它们的结构，并评估了它们对Na + 、K( + )-ATP酶上洋地黄受体的结合亲和力。这些衍生物的亲和力低于母体化合物。α位的亲水性羟基比β位的羟基对亲和力的损害更大。
