1997•PubMedRequires access
Hypnotic activities of N3-benzyl and xylyl substituted arabinofuranosyluracil.
Toshiyuki Kimura, Chun Ys, M. IKEDA, Kiyofumi KOBANA, Kyoihci A. Watanabe, Shigemi Kondo, I K Ho, Izumi Yamamoto
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Abstract
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.