Mutation Information
Mutation Site
|
K103N |
Mutation Type
|
Amino acid level |
Gene/Protein/Region Type
|
RT |
Literature Information
PubMed PMID
|
32140396
|
Published Year
|
2020 |
Journal
|
Acta pharmaceutica Sinica. B |
Title
|
Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors. |
Author
|
Wu Y,Tang C,Rui R,Yang L,Ding W,Wang J,Li Y,Lai CC,Wang Y,Luo R,Xiao W,Zhang H,Zheng Y,He Y |
Evidence
|
The most promising compound DB02 exhibited potent anti-HIV-1 activity against laboratory adapted strains and primary isolated strains (EC50s (concentrations inhibiting virus replication by 50%) range from 2.40 to 41.8 nmol/L), along with an improved sensitivity against K103N or Y181C than S-DABOs26.
|
|
|