发明授权
US5593999A Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT) 失效
甘氨酰胺核糖核苷酸甲酰转移酶(GARFT)的非经典叶酸类似物抑制剂

Non-classical folate analogue inhibitors of glycinamide ribonucleotide
formyltransferase (GARFT)
摘要:
Several new 10-formyl and 10-hydroxymethyl derivatives of 5,8,10-trideazapteroic acid are provided, as well as procedures for their preparation. These compounds were shown to be powerful inhibitors of glycinamide ribonucleotide formyltransferase (GARFT), an enzyme that mediates the de novo biosynthesis of purine nucleotides that are required for DNA synthesis and cell division. Due to their ability to interfere with nucleotide biosynthesis and to penetrate microbial cells they are potential anti-microbial agents and are useful for the treatment of opportunistic infections in AIDS and other infections caused by micro-organisms that are resistant to conventional anti-bacterial and anti-fungal agents.
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