Fujii T, Walker G C, Leonard N J
J Med Chem. 1979 Feb;22(2):125-9. doi: 10.1021/jm00188a003.
The direct alkylation of adenine at the 3 position has been extended to produce series of 3-alkyl-, 3-allyl-, and 3-(substituted benzyl)adenines. When these compounds were tested for enzyme inhibition and antiviral activity in vitro, 3-n-pentyladenine was found to be the most active compound in inhibiting the enzyme dopamine-beta-hydroxylase, and 3-(2-bromobenzyl)adenine showed the most striking inhibition of multiplication of Vaccinia virus and of Herpes simplex virus in tissue culture.
腺嘌呤在3位的直接烷基化反应已得到扩展,以制备一系列3-烷基、3-烯丙基和3-(取代苄基)腺嘌呤。当对这些化合物进行体外酶抑制和抗病毒活性测试时,发现3-正戊基腺嘌呤是抑制多巴胺-β-羟化酶最具活性的化合物,而3-(2-溴苄基)腺嘌呤在组织培养中对痘苗病毒和单纯疱疹病毒的增殖表现出最显著的抑制作用。