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为了寻找心血管系统药物,以表雄酮为原料,合成了7个16,17位取代的目标化合物:2β-(4’-甲基-1’-哌嗪基)-3α-羟基-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α-羟基-16α-溴-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-氧-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-肟-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17β-氨基-5α-雄甾烷和2β—(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-16β-氨基-5α-雄甾烷。初步药理试验结果表明它们都有不同程度的抗心律失常活性。
In order to find a cardiovascular system drug, seven 16,17-substituted target compounds were synthesized from epiandrosterone: 2β- (4’-methyl-1’-piperazinyl) -3α-hydroxy-5α- 2β- (4’-methyl-1’-piperazinyl) -3α, 17β-dihydroxy-5α-androstane, 2β- (4’-methyl- (4’-methyl-1’-piperazinyl) -3α, 16α-dihydroxy-17-oxo-5α -androstane, 2β- (4’-methyl-1’-piperazinyl) -3α, 16α- dihydroxy-17-oxime-5α- androstane, 2β- (4’-methyl- -piperazinyl) -3α, 16α-dihydroxy-17β-amino-5α-androstane and 2β- (4’-methyl-1’-piperazinyl) -3α, 17β-dihydroxy-16β-amino -5α-androstane. Preliminary pharmacological test results show that they have varying degrees of anti-arrhythmic activity.