Tricyclic purine analogues as antiparasitic and antiviral agents.

摘要

Purine antimetabolites have been very successful therapeutic agents against a host of infectious diseases and malignancies. As much as successful treatment relies on the efficient accumulation by the target cell or organism, it highly relies on selective action on a vital biochemical pathway of the target cell. Here we design and synthesize a new class of thieno-separated tricyclic purine nucleoside and nucleobases (1–10). Their ability to interact with transporters from human erythrocytes or Trypanosoma brucei is reported herein. We report that these compounds display remarkable selectivity for the parasite's transporters. They have also shown a significant interaction with the transporters of Leishmania major. Furthermore, the antiviral activity of some of the compounds was promising.*; *Please refer to dissertation for diagrams.