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Published on: March 20, 2018
Synthesis and Evaluation of Nifurtimox-Adamantane Adducts with Trypanocidal Activity
Angeliki-Sofia Foscolos1, Ioannis Papanastasiou1, Andrew Tsotinis1
1School of Health Sciences, Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 157 84, Athens, Greece.
Abstract:
The synthesis and pharmacological evaluation of C1-substituted adamantane hydrazones, their C2-substituted isomers, and C1-substituted adamantane furanoic carboxamides is described. These new adamantane derivatives exhibited an interesting pharmacological profile in terms of trypanocidal activity and selectivity. The most active adduct with the best selectivity in this study was found to be the phenylacetoxy hydrazone 1 b (2-[4-(tricyclo[3.3.1.13,7 ]dec-1-yl)phenyl]-N'-[(5-nitrofuran-2-yl)methylene]acetohydrazide; EC50 =11±0.9 nm, SITb =770).
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