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• W2026590908 abstract "Cost and toxicity problems associated with highly active antiretroviral therapy (HAART) in HIV/AIDS treatment could be alleviated by using designed multiple ligands (DMLs). Dual inhibitors of HIV reverse transcriptase (RT) and integrase (IN) were rationally designed by introducing a diketoacid (DKA) functionality into the tolerant C-5 site of RT inhibitor delavirdine. The resulting compounds all demonstrate good activity against both RT and IN in enzymatic assays and HIV in cell-based assay, whereas their C-7 regioisomers are all inactive in these assays. Balanced activities were observed with C-3 halogenated inhibitors." @default.
• W2026590908 created "2016-06-24" @default.
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• W2026590908 creator A5036830700 @default.
• W2026590908 date "2008-04-01" @default.
• W2026590908 modified "2023-10-14" @default.
• W2026590908 title "Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: Introducing a diketoacid functionality into delavirdine" @default.
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• W2026590908 doi "https://doi.org/10.1016/j.bmc.2008.02.007" @default.
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