1．6-二-(N^5-取代苯基-N^1-二胍)己烷盐酸盐的合成和体外抗菌活性

Synthesis and in vitro antibacterial activity of 1,6-Di-(N^5-phenyl-N^1-diguanido) hexane dihydrochloride

为寻找高效、低毒的新一代双胍类抗菌药物,根据电子等排原理,设计并用新的合成方法合成了五种1.6-二-(N5-取代苯基-N1-二胍)己烷双胍类化合物盐酸盐,其中四种为未见文献报道的新化合物,其结构经1HNMR,13CNMR,IR等方法确证.生物活性实验结果表明,部分化合物具有较强的抗菌作用,并对其构效关系进行了探讨.毒性实验表明化合物是低毒的.

In order to find new agents of antibacterial bis-bignanides with high antibacterial activities and low toxicity, five compounds of 1,6-di-（N^5-phenyl-N^1 -diguanido） hexane dihydrochloride were designed and synthesized by the modified synthetic method reported in the literature according to biological isosterism, of which four compounds have not been reported until now. Compound structures were determined by IR, 1^HNMR, and 13^CNMR. The biological activity tests show that some compounds have good antibacterial activity in vitro, and toxicity tests show that compounds have low toxicity. The structure-activity relationship was discussed.