| Literature DB >> 31066972 |
Angeliki-Sofia Foscolos1, Ioannis Papanastasiou1, Andrew Tsotinis1, Martin C Taylor2, John M Kelly2.
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).Entities:
Keywords: 4-(adamant-1-yl)phenyl substitution; 4-(adamant-2-yl)phenyl substitution; hydrazones; nifurtimox; trypanocidal activity
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Year: 2019 PMID： 31066972 DOI： 10.1002/cmdc.201900165
Source DB: PubMed Journal: ChemMedChem ISSN： 1860-7179 Impact factor: 3.466