Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)
| Autor: | Robert K. Campbell, Michael P. Pollastri, Jennifer L. Woodring, Nicholas D. Bland, Stefan O. Ochiana |
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| Rok vydání: | 2013 |
| Předmět: |
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Molecular Pyridines Clinical Biochemistry Trypanosoma brucei brucei Catechols Protozoan Proteins Pharmaceutical Science Trypanosoma brucei Pharmacology Biochemistry Article chemistry.chemical_compound Phosphodiesterase-4 Drug Discovery medicine Humans African trypanosomiasis Molecular Biology Trypanocidal agent Catechol biology Drug discovery Organic Chemistry Phosphodiesterase biology.organism_classification medicine.disease Trypanocidal Agents Trypanosomiasis African chemistry 3' 5'-Cyclic-AMP Phosphodiesterases Benzamides Molecular Medicine Phosphodiesterase 4 Inhibitors Piclamilast |
| Zdroj: | Bioorganicmedicinal chemistry letters. 23(21) |
| ISSN: | 1464-3405 |
| Popis: | Human African trypanosomiasis (HAT) is a parasitic neglected tropical disease that affects 10,000 patients each year. Current treatments are sub-optimal, and the disease is fatal if not treated. Herein, we report our continuing efforts to repurpose the human phosphodiesterase 4 (hPDE4) inhibitor piclamilast to target trypanosomal phosphodiesterase TbrPDEB1. We prepared a range of substituted heterocyclic replacements for the 4-amino-3,5-dichloro-pyridine head group of piclamilast, and found that these compounds exhibited weak inhibitory activity of TbrPDEB1. |
| Databáze: | OpenAIRE |
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