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Org Biomol Chem. 2012 Dec 7;10(45):8985-93. doi: 10.1039/c2ob26439k. Epub 2012 Oct 16.

Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay.

Author information

1
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.

Abstract

Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.

PMID:
23070233
DOI:
10.1039/c2ob26439k
[Indexed for MEDLINE]

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