Mutation Information
Mutation Site
|
Q148H |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
IN |
Combined Mutation
|
in.Q148H+in.G140S |
Relevant Drug
|
raltegravir (RAL);elvitegravir (EVG) |
Literature Information
PubMed PMID
|
32389483
|
Published Year
|
2020 |
Journal
|
Bioorganic & medicinal chemistry |
Title
|
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors. |
Author
|
Patel M,Naidu BN,Dicker I,Higley H,Lin Z,Terry B,Protack T,Krystal M,Jenkins S,Parker D,Panja C,Rampulla R,Mathur A,Meanwell NA,Walker MA |
Evidence
|
The [3.2.2]-bridged tricyclic system was identified as an advantageous chemotype, with representatives exhibiting excellent antiviral activity against both wild-type viruses and the G140S/Q148H resistant virus that arises in response to therapy with raltegravir and elvitegravir.
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