Potential Antileishmanial Activity of 4-N-Acylhydrazone Pyrazolo[3,4-d]pyridazin-7-ones: Synthesis, in vitro Biological Evaluations and Computational Studies
| Autor: | Maria Helena Sarragiotto, Julia Poletto, Gessica M. Ribeiro, Danielle Lazarin Bidóia, Fávero Reisdorfer Paula, Michael J. V. da Silva, Andrey P. Jacomini, Jéssica T.C. Yokoyama, Celso Vataru Nakamura, Fernanda A. Rosa |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
pyrazolo[3
4-d]pyridazinone biology 010405 organic chemistry Chemistry Stereochemistry In silico N-acylhydrazone General Chemistry 010402 general chemistry biology.organism_classification 01 natural sciences In vitro 0104 chemical sciences medicine.anatomical_structure medicine Selectivity Axenic Cytotoxicity Fibroblast Amastigote IC50 Leishmania amazonensis |
| Zdroj: | Journal of the Brazilian Chemical Society v.29 n.12 2018 Journal of the Brazilian Chemical Society Sociedade Brasileira de Química (SBQ) instacron:SBQ Journal of the Brazilian Chemical Society, Volume: 29, Issue: 12, Pages: 2657-2668, Published: DEC 2018 |
| Popis: | In this work a series of 28 novel pyrazolo[3,4-d]pyridazin-7-ones were synthesized and tested against Leishmania amazonensis (strain WHOM/BR/75/JOSEFA) in promastigote and axenic amastigote forms. Five compounds were active against both cellular forms with IC50 (inhibitory concentration growth of 50%) values of 20.2, 11.7, 16.2, 29.5 and 40.3 µM for promastigote and 17.4, 25.2, 3.84, 21.8 and 22.7 µM for axenic amastigote. All compounds were studied by the Lipinski rule, cytotoxicity both in silico and in vitro to fibroblast line (L929) and macrophages (J774A1), and the most active compound showed a selectivity index of 59.9. |
| Databáze: | OpenAIRE |
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