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BMS Derivatives C7-Linked to β-Cyclodextrin and Hyperbranched Polyglycerol Retain Activity against R5-HIV-1NLAD8 Isolates and Can Be Deemed Potential Microbicides
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Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine,which are related to entry inhibitors developed by Bristol-MyersSquibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring.These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions.Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5HIV-1NLAD8 isolates.Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time.
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PETIT ROIG, Elena, BOSCH HEREU, Lluís, COSTA I ARNAU, Anna m., RODRÍGUEZ-IZQUIERDO, Ignacio, SEPÚLVEDA-CRESPO, Daniel, MUÑOZ-FERNÁNDEZ, M. angeles, VILARRASA I LLORENS, Jaume. BMS Derivatives C7-Linked to β-Cyclodextrin and Hyperbranched Polyglycerol Retain Activity against R5-HIV-1NLAD8 Isolates and Can Be Deemed Potential Microbicides. _ChemMedChem_. 2021. Vol. 16, núm. 14, pàgs. 2217-2222. [consulta: 25 de febrer de 2026]. ISSN: 1860-7179. [Disponible a: https://hdl.handle.net/2445/186028]