4.5 Review

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

Journal

CHEMMEDCHEM
Volume 16, Issue 5, Pages 743-766

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202000695

Keywords

AIDS; HIV-1; NRTI; nucleoside analogues; reverse transcriptase inhibitors

Funding

  1. AMED [JP20fk0310102, JP20am0401008, JP20ak0101119]
  2. JST-CREST [JPMJCR18S1]
  3. Takeda Science Foundation

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Despite the availability of various anti-HIV drugs, NRTIs remain widely used and of interest. However, HIV has developed resistance against NRTIs, necessitating the search for novel therapies to combat the virus.
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), which 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.

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