Structure, Synthesis and Inhibition Mechanism of Nucleoside Analogues as HIV-1 Reverse Transcriptase Inhibitors (NRTIs).

Yoshida, Yuki; Honma, Masakazu; Kimura, Yasuaki; Abe, Hiroshi

Acquired immunodeficiency syndrome (AIDS) is caused by infection with the human immunodeficiency virus (HIV). Although treatments against HIV infection are available, AIDS remains a serious disease that causes many deaths annually. Although a variety of anti-HIV drugs have been synthesized and marketed to treat HIV infected patients, nucleoside analogue reverse transcriptase inhibitors (NRTIs) that mimic nucleosides are used extensively and remain a subject of interest to medicinal chemists. However, HIV has acquired drug resistance against NRTIs and thus the struggle to find novel therapies continues. In this review, we trace the trajectory of NRTIs, focusing on the synthesis, mechanisms of action and applications of NRTIs that have been developed.