AI Article Synopsis
- A series of eight heterodimers were designed to inhibit HIV replication by combining a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and an Integrase Inhibitor (INI) using a linker.
- Among the selected NRTIs were d4U, d2U, and d4T, while the INIs chosen were specific beta-diketo acids.
- The two classes of inhibitors were linked using an amino acid (either glycine or beta-alanine) to create a compound that could potentially enhance HIV therapy.
Article Abstract
Selected for their expected ability to inhibit HIV replication, a series of eight heterodimers containing a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and an Integrase Inhibitor (INI), bound by a linker, were designed and synthesized. For the NRTIs, d4U, d2U and d4T were chosen. For the INIs, 4-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxobutyric acid (6) and 4-(3,5-dibenzyloxyphenyl)-2,4-dioxobutyric acid (9) (belonging to the beta-diketo acids class) were chosen. The conjugation of the two different inhibitors (NRTI and INI) was performed using an amino acid (glycine or beta-alanine) as a cleavable linker.
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| http://dx.doi.org/10.1080/14756360412331280554 | DOI Listing |
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