Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 86, Issue 4, Pages 614-618Publisher
WILEY
DOI: 10.1111/cbdd.12524
Keywords
antiviral activity; click chemistry; drug design; HIV; NNRTIs; pyrimidine; SAR
Funding
- National Natural Science Foundation of China (NNSFC) for International Cooperation [81420108027]
- National Natural Science Foundation of China [81102320, 81273354]
- Research Fund for the Doctoral Program of Higher Education of China [20110131130005, 20110131120037]
- Science and Technology Development Project of Shandong Province [2014GSF118012]
- China Postdoctoral Science Foundation [2012T50584]
- KU Leuven [GOA 10/014]
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A series of novel S-DABO derivatives with the substituted 1,2,3-triazole moiety on the C-2 side chain were synthesized using the simple and efficient CuAAC reaction, and biologically evaluated as inhibitors of HIV-1. Among them, the most active HIV-1 inhibitor was compound 4-((4-((4-(2,6-dichlorobenzyl)-5-methyl-6-oxo-1,6-dihydropyrimidin-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)methyl)benzenesulfonamide (B5b7), which exhibited similar HIV-1 inhibitory potency (EC50= 3.22m) compared with 3TC (EC50=2.24m). None of these compounds demonstrated inhibition against HIV-2 replication. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed briefly.
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