Avila J L, Polegre M A, Avila A, Robins R K
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1986;83(2):285-9. doi: 10.1016/0742-8413(86)90124-6.
The capacity of 54 different pyrazolo-(3,4-d)- or -(4,3-d)-pyrimidine derivatives to inhibit American Leishmania promastigote multiplication was evaluated. Among pyrazolo-(3,4-d)-pyrimidines, eight derivatives showed leishmanistatic activity, 4-aminopyrazolo-(3,4-d)-pyrimidine (APP) being the most active, about eight-fold more than 4-hydroxy-pyrazolo-(3,4-d)-pyrimidine (HPP). 7-Hydroxy-3-beta-D-ribofuranosylpyrazolo-(4,3-d)-pyrimidine (FoB) was as active as 7-amino-3-beta-D-ribofuranosylpyrazolo-(4,3-d)-pyrimidine (FoA), a situation different to that found for pyrazolo-(3,4-d)-pyrimidines. Furthermore, different chemical modifications in formycin structure did not modify inhibitory effects. It can be concluded that regarding American Leishmania the chemical analogy to hypoxanthine or inosine of pyrazolo-(3,4-d)- and pyrazolo-(4,3-d)-pyrimidine, respectively, is not absolutely critical, as different modifications on the heterocyclic ring did not abolish the inhibitory activity of these compounds.
评估了54种不同的吡唑并-(3,4 - d)-或-(4,3 - d)-嘧啶衍生物抑制美洲利什曼原虫前鞭毛体增殖的能力。在吡唑并-(3,4 - d)-嘧啶中，8种衍生物表现出抗利什曼活性，4 - 氨基吡唑并-(3,4 - d)-嘧啶（APP）活性最强，比4 - 羟基吡唑并-(3,4 - d)-嘧啶（HPP）活性约高8倍。7 - 羟基 - 3 - β - D - 呋喃核糖基吡唑并-(4,3 - d)-嘧啶（FoB）与7 - 氨基 - 3 - β - D - 呋喃核糖基吡唑并-(4,3 - d)-嘧啶（FoA）活性相当，这与吡唑并-(3,4 - d)-嘧啶的情况不同。此外，间型霉素结构的不同化学修饰并未改变抑制效果。可以得出结论，对于美洲利什曼原虫而言，吡唑并-(3,4 - d)-和吡唑并-(4,3 - d)-嘧啶分别与次黄嘌呤或肌苷的化学相似性并非绝对关键，因为杂环上的不同修饰并未消除这些化合物的抑制活性。
