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Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
Author: ChenFen-Er, De ClercqErik, HanSheng, PannecouqueChristophe, SangYali, TaoYuan, WuYan, ZhuangChunlin
Original Abstract of the Article :
The fragment hopping approach is widely applied in drug development. A series of diarylpyrimidines (DAPYs) were obtained by hopping the thioacetamide scaffold to novel human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitors (NNRTIs) to address the cytotoxicity issu...See full text at original site
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* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。
引用元：
https://doi.org/10.1016/j.ejmech.2019.111874
データ提供：米国国立医学図書館（NLM）
Fragment Hopping: A Novel Approach to Combatting HIV-1
HIV-1, a virus that causes AIDS, continues to be a global health challenge. This research explores a novel approach to developing new drugs against HIV-1, using a technique called 'fragment hopping.' The authors sought to address the cytotoxicity issue associated with existing HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) by modifying the molecular structure of these drugs. This is like exploring a vast desert and seeking a new path that circumvents treacherous obstacles, ultimately leading to a safer and more effective route to combating the virus.
A New Path: Fragment Hopping for Improved Efficacy
The study successfully identified a new class of NNRTIs with improved anti-viral activity and reduced cytotoxicity. This is a significant breakthrough in the fight against HIV-1, offering a promising path for developing new drugs with better safety profiles. The study also highlights the importance of computational modeling in drug discovery, enabling researchers to predict the binding behavior of new compounds and guide the development process.
Navigating the Desert of Drug Development: Toward a Cure
This research presents a promising new approach to combating HIV-1. Fragment hopping offers a path for developing more effective and safer drugs, potentially leading to improved treatment options for patients. Continued research and development in this area are essential to achieving the ultimate goal of a cure for HIV-1, paving the way for a healthier future.
Dr.Camel's Conclusion
This study presents a promising new approach to developing more effective and safer drugs against HIV-1. The innovative 'fragment hopping' technique has the potential to revolutionize drug discovery and offer new hope for patients. This research is a testament to the power of scientific innovation in our ongoing quest to combat this formidable virus.
Date :
- Date Completed 2020-02-18
- Date Revised 2020-02-18
Further Info :
Related Literature
English
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