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Volume 23, Issue 1
  • ISSN: 2211-3525
  • E-ISSN: 2211-3533

Abstract

Introduction

HIV utilizes a reverse transcriptase (RT) enzyme to convert the HIV-RNA into DNA. Inhibition of the reverse transcription mechanism of HIV-RT may serve as a potential therapeutic approach to impede the proliferation of HIV in those who are infected. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a type of medication that directly and non-competitively bind to the allosteric site of HIV-RT, inhibiting its polymerase activity.

Aim

This study was aimed at the synthesis of hydrazine derivatives and their evaluation for HIV- reverse transcriptase inhibition using RT-qPCR-based assay.

Objective

The objective of this study was to determine the HIV- reverse transcriptase inhibition using chemical compounds as non-nucleoside reverse transcriptase inhibitors in RT-qPCR.

Methods

This study involved the synthesis of five distinct hydrazine derivatives, which were subsequently tested for their capacity to inhibit HIV-RNA polymerization by targeting HIV-derived reverse transcriptase. For the determination of the study assay, commercially available HIV-RT was subjected to treatment with derivatives and utilized in an RT-qPCR experiment to determine the activity or inhibitory effects of HIV-RT for HIV-RNA polymerization.

Results

The assay results demonstrated a reduction in viral load due to suppression of reverse transcriptase activity when compared to the pre-quantified values obtained from untreated RT. Among the five compounds, 4-N, N-dimethylamino benzaldehyde hydrazine (CHN) had the highest ability to suppress HIV-RT. This molecule reduced HIV-RNA reverse transcription by more than 90% during RT-qPCR, which is a novel and promising strategy.

Conclusion

N, N-dimethylamino benzaldehyde hydrazine (CHN) can suppress the activity of HIV-RT, and this effect becomes more pronounced as the concentration of the compound increases.

© 2025 Bentham Science Publishers
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2024-06-03
2025-01-28

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In-vitro Study of HIV-derived Reverse Transcriptase Inhibition
Anti Infect. Agents 23, E030624230615 (2025); https://doi.org/10.2174/0122113525287587240515044540
/content/journals/aia/10.2174/0122113525287587240515044540
/content/journals/aia/10.2174/0122113525287587240515044540
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  • Article Type:     Research Article
Keyword(s): HIV; hydrazine derivatives; inhibition; non-nucleoside reverse transcriptase inhibitors; reverse transcriptase; RT-qPCR assay

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