Gosselin G, Bergogne M C, De Rudder J, De Clercq E, Imbach J L
J Med Chem. 1987 Jun;30(6):982-91. doi: 10.1021/jm00389a005.
The alpha- and beta-D-lyxofuranosyl analogues of the naturally occurring nucleosides have been synthesized and their antiviral properties examined. The alpha anomers were prepared by glycosylation of purine and pyrimidine aglycons with tetra-O-acetyl-alpha-D-lyxofuranose, followed by removal of the blocking groups. The beta anomers were obtained by sequential oxidation and reduction of 3',5'-O-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl)-beta-D-x ylofuranosyl nucleosides. The lyxofuranosyl nucleosides were tested for their activity against a variety of RNA and DNA viruses and for inhibition of cell growth. One compound, 9-alpha-D-lyxofuranosyladenine, showed activity against herpes simplex virus types 1 and 2 both in vitro and in vivo.
已合成天然核苷的α-和β-D-呋喃来苏糖基类似物，并对其抗病毒特性进行了研究。α异头物通过嘌呤和嘧啶苷元与四-O-乙酰基-α-D-呋喃来苏糖进行糖基化反应制备，随后除去保护基团。β异头物通过对3',5'-O-(1,1,3,3-四异丙基二硅氧烷-1,3-二基)-β-D-呋喃木糖基核苷进行连续氧化和还原反应获得。对呋喃来苏糖基核苷针对多种RNA和DNA病毒的活性以及对细胞生长的抑制作用进行了测试。一种化合物，即9-α-D-呋喃来苏糖基腺嘌呤，在体外和体内均显示出对1型和2型单纯疱疹病毒的活性。
