Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Author: DaelemansDirk, De ClercqErik, DingXiao, FangZengjun, HuangBoshi, HuoZhipeng, KangDongwei, LiuXinyong, LuXueyi, MengQing, PannecouqueChristophe, TianYe, WuGaochan, XuHaoran, YuZhao, ZhanPeng, ZhangHeng, ZhouZhongxia

Paper Details 
Original Abstract of the Article :
This work follows on from our initial discovery of a series of piperidine-substituted thiophene[3,2-d]pyrimidine HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTI) ( J. Med. Chem. 2016 , 59 , 7991 - 8007 ). In the present study, we designed, synthesized, and biologically tested several se...See full text at original site
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引用元:
https://doi.org/10.1021/acs.jmedchem.7b00332

データ提供:米国国立医学図書館(NLM)

A New Oasis in the Desert of HIV Treatment: Optimizing Thiophene[3,2-d]pyrimidine Derivatives

The fight against [HIV-1 infection] is a relentless journey, much like a caravan traversing a vast desert. This study, like a team of skilled chemists exploring new pathways, investigates the potential of [thiophene[3,2-d]pyrimidine derivatives] as [potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)]. The research seeks to develop new drugs that are more effective against HIV and less susceptible to resistance mutations, potentially offering a new weapon in the battle against this devastating virus.

A Promising Oasis: Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs

This research, like a caravan discovering a new oasis in a barren desert, offers a promising new approach to [HIV-1 treatment]. The findings indicate that [thiophene[3,2-d]pyrimidine derivatives] have the potential to be highly effective against HIV, exhibiting [single-digit nanomolar anti-HIV potencies]. This discovery, like a hidden well in the desert, could lead to new drugs that are more effective against HIV and less susceptible to resistance mutations.

Navigating the Landscape: Developing a New Generation of HIV Drugs

This research, like a map guiding a caravan through a challenging landscape, highlights the need for a new generation of HIV drugs that are more effective and less susceptible to resistance. The findings suggest that [thiophene[3,2-d]pyrimidine derivatives] could be a promising candidate for such drugs, potentially offering a new path toward controlling HIV infection. Further research, much like a continued exploration of a vast desert, is needed to fully understand the long-term efficacy, safety, and pharmacokinetic properties of these derivatives.

Dr.Camel's Conclusion

The research on thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs offers a glimmer of hope, like a star shining brightly in the desert night. This study suggests that these derivatives could be a valuable new tool in the fight against HIV, potentially offering a more effective and durable approach to treatment. While further research is needed to confirm their efficacy and safety, this research offers a potential new path for individuals living with HIV, much like a caravan discovering a new route through a vast and challenging desert.

Date :
  1. Date Completed 2017-06-19
  2. Date Revised 2018-12-30
Further Info :

Pubmed ID

28481112

DOI: Digital Object Identifier

10.1021/acs.jmedchem.7b00332

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