Synthesis and Evaluation of Nifurtimox-Adamantane Adducts with Trypanocidal Activity

被引：8

作者：

Foscolos, Angeliki-Sofia ^{[1
]}

Papanastasiou, Ioannis ^{[1
]}

Tsotinis, Andrew ^{[1
]}

Taylor, Martin C. ^{[2
]}

Kelly, John M. ^{[2
]}

机构：

[1] Univ Athens, Div Pharmaceut Chem, Sch Hlth Sci, Athens 15784, Greece

[2] London Sch Hyg & Trop Med, Dept Pathogen Mol Biol, Keppel St, London WC1E 7HT, England

来源：

CHEMMEDCHEM | 2019年 / 14卷 / 13期

关键词：

4-(adamant-1-yl)phenyl substitution; 4-(adamant-2-yl)phenyl substitution; hydrazones; nifurtimox; trypanocidal activity; RECEPTOR-BINDING-AFFINITY; DERIVATIVES; DESIGN;

D O I：

10.1002/cmdc.201900165

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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[3.3.1.1(3,7)]dec-1-yl)phenyl]-N '-[(5-nitrofuran-2-yl)methylene]acetohydrazide; EC50=11 +/- 0.9 nm, SITb=770).

引用

页码：1227 / 1231

页数：5

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