1098099-99-0Relevant articles and documents
α-D-Mannoside ligands with a valency ranging from one to three: Synthesis and hemagglutination inhibitory properties
Al-Mughaid, Hussein,Khazaaleh, Maha
, (2021)
Six mono-, di-, and trivalent α-D-mannopyranosyl conjugates built on aromatic scaffolds were synthesized in excellent yields by Cu(I) catalyzed azide-alkyne cycloaddition reaction (CuAAC). These conjugates were designed to have unique, flexible tails that combine a mid-tail triazole ring, to interact with the tyrosine gate, with a terminal phenyl group armed with benzylic hydroxyl groups to avoid solubility problems as well as to provide options to connect to other supports. Biological evaluation of the prepared conjugates in hemagglutination inhibition (HAI) assay revealed that potency increases with valency and the trivalent ligand 6d (HAI = 0.005 mM) is approximately sevenfold better than the best meta-oriented monovalent analogues 2d and 4d (HAI ≈ 0.033 mM) and so may serve as a good starting point to find new lead ligands.
Efficient macrocyclization achieved via conformational control using intermolecular noncovalent π-cation/arene interactions
Bolduc, Philippe,Jacques, Alexandre,Collins, Shawn K.
supporting information; experimental part, p. 12790 - 12791 (2010/11/04)
Quinolinium salt 3 is an effective additive that acts as a conformation control element (CCE) to promote macrocyclization to form rigid cyclophanes via olefin metathesis or Glaser-Hay coupling, which do not cyclize in the absence of the additive. The additives are easily synthesized and highly modifiable and have solubility profiles which allow for simple recovery via filtration.
