Schneller S W, Thompson R D, Cory J G, Olsson R A, De Clercq E, Kim I K, Chiang P K
J Med Chem. 1984 Jul;27(7):924-8. doi: 10.1021/jm00373a020.
A two-step synthesis of 8-amino-3-beta-D-ribofuranosyl-1,2,4-triazolo[4,3-a]pyrazine (3), which is an isomer of formycin that resembles 3-deazaadenosine, is reported. Compound 3 is also described as as being a very poor substrate for adenosine deaminase and to be both a competitive and an irreversible inhibitor of S-adenosylhomocysteinase in the synthesis direction. L1210 cell growth in culture was inhibited by 3. Compound 3 was not converted to the nucleotide level in erythrocytes but was found to inhibit both the cellular uptake of nucleic acid precursors and their incorporation into the nucleic acids of L1210 cells. Finally, 3 was found to be a weak antiviral agent and coronary vasodilator.
报道了8-氨基-3-β-D-呋喃核糖基-1,2,4-三唑并[4,3-a]吡嗪（3）的两步合成方法，该化合物是间型霉素的异构体，类似于3-脱氮腺苷。化合物3也被描述为腺苷脱氨酶的极差底物，并且在合成方向上是S-腺苷同型半胱氨酸酶的竞争性和不可逆抑制剂。3抑制培养中的L1210细胞生长。化合物3在红细胞中未转化为核苷酸水平，但被发现抑制核酸前体的细胞摄取及其掺入L1210细胞的核酸中。最后，发现3是一种弱抗病毒剂和冠状血管扩张剂。
