Weier R M, Hofmann L M
J Med Chem. 1976 Jul;19(7):975-7. doi: 10.1021/jm00229a025.
The synthesis and antimineralocorticoid potencies of several steroidal spirolactones bearing novel nitrogenous substituents in the 7alpha position are reported. These substituents include the cyano, the isocyanato, and the alkoxycarbonylamino groupings. The nitrile 1b and the N-carbomethoxy compound 1h showed good antimineralocorticoid potency (MED less than or equal to 0.79 mg) on subcutaneous administration to adrenalectomized rats.
报道了几种在7α位带有新型含氮取代基的甾体螺内酯的合成及其抗盐皮质激素活性。这些取代基包括氰基、异氰酸酯基和烷氧羰基氨基基团。腈1b和N-甲氧羰基化合物1h对肾上腺切除的大鼠皮下给药时显示出良好的抗盐皮质激素活性(最小有效剂量小于或等于0.79毫克)。