BMS Derivatives C7-Linked to β-Cyclodextrin and Hyperbranched Polyglycerol Retain Activity against R5-HIV-1

Autor:	Elena, Petit, Lluís, Bosch, Anna M, Costa, Ignacio, Rodríguez-Izquierdo, Daniel, Sepúlveda-Crespo, M Angeles, Muñoz-Fernández, Jaume, Vilarrasa
Rok vydání:	2021
Předmět:	Glycerol Structure-Activity Relationship Dose-Response Relationship Drug Molecular Structure Anti-HIV Agents HIV Fusion Inhibitors Polymers beta-Cyclodextrins HIV-1 Humans Amides HIV Reverse Transcriptase
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:	https://explore.openaire.eu/search/publication?articleId=pmid________::f402e65d678f6ad0ee6edd87fd819f81 https://pubmed.ncbi.nlm.nih.gov/33843142 Zobrazit plný text záznamu Plný text