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Recent Advances on the Role of Nitrogen-Based Heterocyclic Scaffolds in Targeting HIV through Reverse Transcriptase Inhibition

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CHEMISTRYSELECT
卷 7, 期 36, 页码 -

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.202202637

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Docking studies; heterocycles; human immunodeficiency virus (HIV); reverse transcriptase (RT); non-nucleoside reverse transcriptase inhibitors (HIV-NNRTI)

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This paper discusses the control of the reverse transcriptase (RT) pathway, the role of heterocyclic compounds in inhibiting the RT pathway, and recent advances in RT inhibitors. The research in this field has provided valuable insights into mechanisms, preclinical and clinical investigations, and structural activity relationships.
Acquired immune deficiency syndrome (AIDS) caused by human immunodeficiency virus continues to scavenge lives of millions around the world. Reverse transcriptase (RT) also known as the RNA-directed DNA polymerase enzyme is responsible for converting RNA into viral DNA through process known as reverse transcription. Investigations on the pathogenic aspects of the RT enzyme, its associated elements such as gag (group-specific antigen gene), pol (polymerase gene), and env (environmental gene) (envelope gene) reveals its contribution towards emergence of resistance to all various anti-HIV drugs. Therefore, research into the control and blockage of the RT pathway has been a prominent focus in the quest for novel targets for HIV treatment. A slew of heterocyclics has been claimed to play a significant part in the fight against doomy HIV, saving the lives of millions of people throughout the world and providing hope for HIV treatment. Due to their improved potency and selectivity, as well as the fact that they have fewer off-target effects against the several targets implicated in RT inhibition, heterocyclics are becoming more and more useful. The RT inhibition pathway, the function of numerous heterocyclic scaffolds, and their ability to inhibit the RT enzyme pathway have all been the main topics of this paper. Recent advances in RT inhibitors in the last eight years (2014-2022) including mechanisms of action, preclinical and clinical investigations, structural activity relationships, and docking studies, to investigate mechanistic studies that would eventually aid in the design and development of powerful RT inhibitors have also discussed.

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