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Mutation Information
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Mutation Site
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L100I |
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Mutation Type
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Amino acid level |
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Gene/Protein/Region Type
|
RT |
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Relevant Drug
|
NNRTIs |
Literature Information
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PubMed PMID
|
32712537
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Published Year
|
2020 |
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Journal
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European journal of medicinal chemistry |
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Title
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Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
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Author
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Chen X,Ding L,Tao Y,Pannecouque C,De Clercq E,Zhuang C,Chen FE |
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Evidence
|
Among all the chiral derivatives, (S)-(-)-12a showed the best potency with the antiviral activities against wild-type (WT) and single mutant strains (L100I, K103 N, Y181C, E138K;especially Y188L), and RT enzyme in the low nanomolar concentration range.
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