Autor: |
Elena, Petit, Lluís, Bosch, Anna M, Costa, Ignacio, Rodríguez-Izquierdo, Daniel, Sepúlveda-Crespo, M Angeles, Muñoz-Fernández, Jaume, Vilarrasa |
Rok vydání: |
2021 |
Předmět: |
|
Zdroj: |
ChemMedChem. 16(14) |
ISSN: |
1860-7187 |
Popis: |
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (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 R5-HIV-1 |
Databáze: |
OpenAIRE |
Externí odkaz: |
|