Kimura T, Chun Y S, Ikeda M, Kobana K, Watanabe K, Kondo S, Ho I K, Yamamoto I
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Nucleic Acids Symp Ser. 1997(37):229-30.
N3-Substituted derivatives of arabinofuranosyluracil (1), methyl (2), ethyl (3), propyl (4), butyl (5), allyl (6), benzyl (7), o-, m-, p-xylyls (8, 9, 10) and alpha-phenethyl (11) derivatives, were synthesized and their CNS depressant effects were evaluated by intracerebroventricular (i.c.v.) injection in mice by using hypnotic activity and pentobarbital-induced sleep prolongation as indices. At a dose of 2.0 mumol/mouse, the values of mean sleeping time induced by 7, 8, 9, and 10 were 144, 154, 117, and 33 min, respectively. Although the alkyl (2-6) derivatives did not cause any hypnotic activity, some derivatives tested (5, 7-10) significantly prolonged the pentobarbital-induced sleeping time.
合成了阿拉伯呋喃糖基尿嘧啶的N3-取代衍生物（1）、甲基（2）、乙基（3）、丙基（4）、丁基（5）、烯丙基（6）、苄基（7）、邻、间、对二甲苯基（8、9、10）和α-苯乙基（11）衍生物，并以催眠活性和戊巴比妥诱导的睡眠时间延长为指标，通过向小鼠脑室内注射来评估它们的中枢神经系统抑制作用。在剂量为2.0 μmol/小鼠时，7、8、9和10诱导的平均睡眠时间分别为144、154、117和33分钟。虽然烷基（2-6）衍生物未引起任何催眠活性，但所测试的一些衍生物（5、7-10）显著延长了戊巴比妥诱导的睡眠时间。
