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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 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 Sida Amides Ciclodextrines AIDS (Disease) Amides Cyclodextrins 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. 2022-05-26T16:55:01Z 2022-05-26T16:55:01Z 2021-04-11 2022-05-26T16:55:02Z info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Versió postprint del document publicat a: https://doi.org/10.1002/cmdc.202100080 ChemMedChem, 2021, vol. 16, num. 14, p. 2217-2222 https://doi.org/10.1002/cmdc.202100080 (c) Wiley-VCH, 2021 info:eu-repo/semantics/openAccess Wiley-VCH Articles publicats en revistes (Química Inorgànica i Orgànica)