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Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1.

Author: ChenFen-Er, ClercqErik De, PannecouqueChristophe, YangYang, ZhuangChunlin

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

A novel series of oxime-biphenyl-DAPYs were designed and synthesized as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) against HIV-1. Compound 7d demonstrated significant activity against both wild-type and mutant strains, with a higher selectivity index than existing FDA-approved drugs.
Paper Details　
Original Abstract of the Article :
Oxime is a key pharmacophore in drug development. The biphenyl diarylpyrimidines (DAPYs) have been developed by our group as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs). In this study, fourteen oxime-biphenyl-DAPYs were designed and synthesized through a privileged scaffold inspir...See full text at original site
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引用元：
https://doi.org/10.1016/j.bioorg.2020.103825

データ提供：米国国立医学図書館（NLM）

Novel Oxime-Biphenyl-DAPYs for HIV-1 Treatment: A Privileged Scaffold Inspired Design

This research delves into the intricate realm of HIV-1 treatment, exploring the potential of novel oxime-biphenyl-DAPYs as potent inhibitors of HIV-1 reverse transcriptase. The study, akin to a desert explorer seeking a hidden oasis of antiviral compounds, investigates the efficacy of these compounds against both wild-type and mutant strains of HIV-1. The authors, driven by the need for effective and safe antiviral therapies, employed a privileged scaffold inspired design strategy to synthesize and evaluate these compounds.

Promising Antiviral Activity of Oxime-Biphenyl-DAPYs

The study reveals the potent antiviral activity of oxime-biphenyl-DAPYs against both wild-type and mutant strains of HIV-1. This is a significant finding, as it suggests that these compounds could potentially overcome resistance to existing anti-HIV drugs.

Developing New Treatment Strategies for HIV-1

This research highlights the potential of oxime-biphenyl-DAPYs as a promising therapeutic strategy for HIV-1. By exploring novel drug candidates and understanding their mechanisms of action, researchers are paving the way for more effective and targeted treatments for HIV-1 infection.

Dr. Camel's Conclusion

This study offers a glimpse into the exciting possibilities of oxime-biphenyl-DAPYs as a potential weapon in the fight against HIV-1. By exploring innovative drug designs and understanding their interaction with viral targets, researchers are steadily advancing towards a future where HIV-1 can be effectively managed.
Date :
  1. Date Completed 2021-03-02
  2. Date Revised 2021-03-02
Further Info :

Pubmed ID

32334191

DOI: Digital Object Identifier

10.1016/j.bioorg.2020.103825

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English

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