Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.

Author: ChenWenmin, DaelemansDirk, De ClercqErik, GaoPing, GinexTiziana, HuangBoshi, JiangXiangyi, KangDongwei, LiZhenyu, LiuXinyong, LuqueFrancisco Javier, PannecouqueChristophe, TianYe, VílchezDavid, ZhanPeng, ZhangJian, ZhaoTong

Paper Details 
Original Abstract of the Article :
Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility. In the present work, hydrophilic morpholine or methylsulfonyl and sulfamide-substituted piperazine/piper...See full text at original site
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引用元:
https://doi.org/10.1021/acs.jmedchem.8b01729

データ提供:米国国立医学図書館(NLM)

Diarylpyrimidine Derivatives: A New Oasis in the Desert of HIV Treatment

HIV, like a persistent drought in the desert, continues to pose a global health challenge. This study, like a tireless caravan seeking a solution, explores the development of new anti-HIV medications, specifically diarylpyrimidine derivatives (DAPYs). The researchers, like skilled desert engineers, carefully design and test these medications, targeting the HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. The study highlights the potential of DAPYs to overcome the challenges posed by HIV drug resistance, offering hope for individuals living with HIV.

A New Route to Treatment: DAPYs' Potential

The study reveals that DAPYs, like a newly discovered water source in the desert, exhibit robust anti-HIV activity against both wild-type and E138K mutant virus. The researchers, like astute desert explorers, identify a promising lead compound (11c), which demonstrates excellent potency and favorable safety profiles, paving the way for further development and optimization of these medications.

Staying Hydrated in the Fight Against HIV: Tips for Patients

Remember, living with HIV, like navigating a harsh desert landscape, requires careful management and adherence to treatment plans. Stay informed about the latest advancements in HIV treatment and work closely with your healthcare provider to develop a personalized plan that meets your specific needs. DAPYs, like a refreshing oasis, offer hope for a more effective and tolerable treatment option, giving individuals living with HIV a chance to thrive.

Dr. Camel's Conclusion

This study, like a shimmering oasis in the desert, provides a glimmer of hope in the fight against HIV. The development of DAPYs, like the discovery of a precious water source, offers a new avenue for treatment, potentially improving outcomes and quality of life for individuals living with HIV. The journey towards a cure continues, and the unwavering dedication of researchers and healthcare professionals provides solace and strength to those affected by this global health challenge.

Date :
  1. Date Completed 2020-03-03
  2. Date Revised 2020-03-03
Further Info :

Pubmed ID

30721060

DOI: Digital Object Identifier

10.1021/acs.jmedchem.8b01729

Related Literature

SNS
PICO Info
in preparation
Languages

English

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