Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi
| Autor: | Paul J. Koovits, Guy Caljon, Charles E. Mowbray, Luiz C. Dias, Louis Maes, Jadel M. Kratz, Marco A. Dessoy, An Matheeussen |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Chagas disease
Trypanosoma cruzi Clinical Biochemistry Pharmaceutical Science Moderate activity Pharmacology 01 natural sciences Biochemistry chemistry.chemical_compound Structure-Activity Relationship Piperidines In vivo Drug Discovery parasitic diseases medicine Structure–activity relationship Animals Humans Chagas Disease Molecular Biology Biology biology 010405 organic chemistry Drug discovery Pharmacology. Therapy Organic Chemistry biology.organism_classification medicine.disease 0104 chemical sciences 010404 medicinal & biomolecular chemistry Chemistry chemistry Molecular Medicine Piperidine Human medicine |
| Zdroj: | Bioorganic and medicinal chemistry letters |
| ISSN: | 1464-3405 0960-894X |
| Popis: | The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline’s recently disclosed open-resource “Chagas box” and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chemistry efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery. |
| Databáze: | OpenAIRE |
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