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从胍乙啶(Ⅰ)和潘必啶(Ⅱ)结构出发,作者设计了β-N-(2,2,6,6-四甲基哌啶)乙胍(Ⅲ_a,BD-31)及其β-N-(2-甲基或顺式2,6-二甲基哌啶)乙胍(Ⅲ_b,BD-37;Ⅲ_c,BD-38)类似物。它们由不同的α-甲基哌啶与氯乙腈生成相应的N-(α-甲基哌啶)乙腈(Ⅷ_(a,b,c)),经氢化锂铝还原变成β-N-(α-甲基哌啶)乙胺(Ⅶ_(a,b,c)),再用硫酸甲基异硫脲引入胍基制得。药理试验发现BD-31,32(Ⅵ),33(Ⅶ_a),38均有明显降压作用,其中以BD-31作用最强。
Starting from the structures of guanethidine (Ⅰ) and pentobarbital (Ⅱ), the authors designed β-N- (2,2,6,6-tetramethylpiperidine) ethanidine (Ⅲ_a, BD-31) N- (2-methyl or cis 2,6-dimethylpiperidine) ethauanidine (III_b, BD-37; III-c, BD-38) analogs. They were prepared from different α-methylpiperidine and chloroacetonitrile to produce the corresponding N- (α-methylpiperidine) acetonitrile (Ⅷ_ (a, b, c) α-methylpiperidine) ethylamine (VII_ (a, b, c)), then the introduction of methyl isothiourea methyl guanidino was prepared. Pharmacological test found BD-31,32 (Ⅵ), 33 (Ⅶ_a), 38 were significantly antihypertensive effect, in which BD-31 strongest.