取代的5,6-二氢-5-硝基尿嘧啶的合成与抗菌评价
Synthesis and antimicrobial evaluation of substituted 5,6-dihydro-5-nitrouracils.
作者信息
Long R A, Matthews T R, Robins R K
出版信息
J Med Chem. 1976 Aug;19(8):1072-4. doi: 10.1021/jm00230a020.
Reaction of 5-nitrouracil derivatives with sodium borohydride in methanol-water, followed by neutralization of the product with acid, has produced 5,6-dihydro-5-nitrouracil (5) 5,6-dihydro-6-dihydro-6-methyl-5-nitrouracil (7), 5,6-dihydro-5-nitro-1-(4-nitrophenyl)uracil (10), and 5,6-dihydro-5-nitro-1(beta-D-ribofuranuronic acid ethyl ester)uracil (12). In assays for antimicrobial activity using strains of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, and Trichophyton mentagrophytes, significant inhibition of growth was not found.
5-硝基尿嘧啶衍生物在甲醇-水体系中与硼氢化钠反应，随后用酸中和产物，得到了5,6-二氢-5-硝基尿嘧啶（5）、5,6-二氢-6-甲基-5-硝基尿嘧啶（7）、5,6-二氢-5-硝基-1-(4-硝基苯基)尿嘧啶（10）和5,6-二氢-5-硝基-1-(β-D-呋喃核糖醛酸乙酯)尿嘧啶（12）。在使用大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌、白色念珠菌和须癣毛癣菌菌株进行的抗菌活性测定中，未发现显著的生长抑制作用。
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