Synthesis and antiplasmodial activity of purine-based -nucleoside analogues.

A series of homologous -nucleoside mimics have been synthesized an efficient and facile synthetic protocol involving the conjugate addition of purine to sugar derived olefinic ester in good yields. The synthesized compounds were evaluated for their antiplasmodial activity against both the CQ-sensitive and resistant strains of . Interestingly, all the synthesized nucleoside analogs exhibited an IC of <5 μM, while compounds , , and showed promising antiplasmodial activity with an IC of 1.61, 0.88, and 1.01 μM against the CQ-sensitive 3D7 strain and 1.14, 1.01, and 2.57 μM against the CQ-resistant K1 strain, respectively.