Development of Simplified Heterocyclic Acetogenin Analogues as Potent and SelectiveTrypanosoma bruceiInhibitors
| Autor: | Terry K. Smith, Marija K. Zacharova, Gordon J. Florence, Stefanie K. Menzies, Lindsay B. Tulloch, Marie I. Thomson, Andrew L. Fraser, Elizabeth F. B. King, Joanne C. Morris, Eoin R. Gould |
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| Rok vydání: | 2016 |
| Předmět: |
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 |
| Zdroj: | Chemmedchem |
| ISSN: | 1860-7179 |
| DOI: | 10.1002/cmdc.201600210 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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