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Your search keyword '"Pyrazolo[3,4-d]pyridazinone"' showing total 1 results
Start Over Descriptor "Pyrazolo[3,4-d]pyridazinone" Topic 010402 general chemistry
1 results on '"Pyrazolo[3,4-d]pyridazinone"'

1. Potential Antileishmanial Activity of 4-N-Acylhydrazone Pyrazolo[3,4-d]pyridazin-7-ones: Synthesis, in vitro Biological Evaluations and Computational Studies

Author

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, and Fernanda A. Rosa

Subjects
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
Abstract

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.

Published
2018

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