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Development of Simplified Heterocyclic Acetogenin Analogues as Potent and SelectiveTrypanosoma bruceiInhibitors
- Source :
- Chemmedchem
- Publication Year :
- 2016
- Publisher :
- Wiley, 2016.
-
Abstract
- Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a burden to human and animal health, having the most devastating effect on the world′s poorest countries. Building upon our previously reported triazole analogues, in this study we describe the synthesis and biological testing of other novel heterocyclic acetogenin‐inspired derivatives, namely 3,5‐isoxazoles, furoxans, and furazans. Several of these compounds maintain low‐micromolar levels of inhibition against Trypanosoma brucei, whilst having no observable inhibitory effect on mammalian cells, leading to the possibility of novel lead compounds for selective treatment.
- Subjects :
- Acetogenins
Stereochemistry
Trypanosoma brucei brucei
trypanosomatids
Trypanosoma brucei
010402 general chemistry
01 natural sciences
Biochemistry
natural product analogues
chemistry.chemical_compound
[3+2] cycloaddition
Oximes
Drug Discovery
Humans
General Pharmacology, Toxicology and Pharmaceutics
Pharmacology
Oxadiazoles
Cycloaddition Reaction
biology
010405 organic chemistry
Drug discovery
Communication
Organic Chemistry
Isoxazoles
biology.organism_classification
Trypanocidal Agents
Communications
0104 chemical sciences
3. Good health
chemistry
Acetogenin
Molecular Medicine
HeLa Cells
Subjects
Details
- ISSN :
- 18607179
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- ChemMedChem
- Accession number :
- edsair.doi.dedup.....2f8e6f1d792dd488a2bb5f1e4565e36c
- Full Text :
- https://doi.org/10.1002/cmdc.201600210