Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors
| Autor: | Antônio Rodolfo de Faria, Marcelo Santos Castilho, Daci José Brondani, Camila Carane Bitencourt Brito, Rafael Matos Ximenes, Ivanildo Mangueira da Silva, Hélder Vinicius Carneiro da Silva, Julianna Ferreira Cavalcanti de Albuquerque |
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| Rok vydání: | 2019 |
| Předmět: |
Biology
01 natural sciences Leishmania braziliensis Superoxide dismutase chemistry.chemical_compound Structure-Activity Relationship Cutaneous leishmaniasis Drug Discovery medicine Humans Enzyme Inhibitors Thiazole Leishmania Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Superoxide Dismutase lcsh:RM1-950 Leishmaniasis General Medicine medicine.disease biology.organism_classification 0104 chemical sciences thermal shift assay 010404 medicinal & biomolecular chemistry Thiazoles lcsh:Therapeutics. Pharmacology Enzyme Drug development chemistry Biochemistry biology.protein thiazole derivatives Brazil Research Paper |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 333-342 (2019) |
| ISSN: | 1475-6374 |
| Popis: | Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites and human host. Despite the differences between SOD of Leishmania braziliensis and human make this enzyme a promising target for drug development efforts. No medicinal chemistry effort has been made to identify LbSOD inhibitors. Herein, we show that thermal shift assays (TSA) and fluorescent protein-labeled assays (FPLA) can be employed as primary and secondary screens to achieve this goal. Moreover, we show that thiazole derivatives bind to LbSOD with micromolar affinity. |
| Databáze: | OpenAIRE |
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