申请人:Zaidan Hojin Biselbutsu Kagaku Kenkyu Kai
公开号:US04163839A1
公开(公告)日:1979-08-07
A novel, unique nucleoside, 3-.beta.-D-ribofuranosyl-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-7-o l, named isocoformycin, of the formula ##STR1## is provided by ring expansion of derivatives of 9-.beta.-D-ribofuranosyl-6-hydroxymethyl-1,6-dihydropurine. Isocoformycin markedly inhibits deaminating enzymes which inactivate formycin and adenine arabinoside (also known as ara-A and Vidarabine). Formycin and adenine arabinoside are used as antiviral and antitumor agents in mammals and birds and isocoformycin is advantageous to prolong the activity and effect of formycin and adenine arabinoside.
提供一种新型独特的核苷酸,命名为异同形酶素(Isocoformycin),化学式为3-.beta.-D-核糖呋喃糖基-3,6,7,8-四氢咪唑[4,5-d][1,3]二氮杂环-7-醇,通过9-.beta.-D-核糖呋喃糖基-6-羟甲基-1,6-二氢嘌呤衍生物的环扩张得到。异同形酶素明显抑制脱氨酶,这种酶会使福尔霉素和腺嘌呤阿拉伯核苷(也称为ara-A和维达拉滨)失活。福尔霉素和腺嘌呤阿拉伯核苷在哺乳动物和鸟类中用作抗病毒和抗肿瘤药物,异同形酶素有利于延长福尔霉素和腺嘌呤阿拉伯核苷的活性和效果。