Bioorganic & Medicinal Chemistry 2015-08-01

Synthesis and evaluation of the anti-nociceptive and anti-inflammatory activity of 4-aminoquinoline derivatives.

Raquel de Meneses Santos, Pooline Rocha Barros, Janaína Heberle Bortoluzzi, Mario Roberto Meneghetti, Yolanda Karla Cupertino da Silva, Amanda Evelyn da Silva, Mariana da Silva Santos, Magna Suzana Alexandre-Moreira

文献索引：Bioorg. Med. Chem. 23 , 4390-6, (2015)

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摘要

In this paper, we describe the synthesis and pharmacological evaluation of a series of 4-aminoquinolines. The compounds were characterised and tested in models of pain and inflammation, using the writhing test with acetic acid, formalin test, peritonitis test by zymosan and arthritis test with Freund's adjuvant complete assay. The results revealed that all of the 4-aminoquinolines that were prepared promoted anti-nociceptive activity as well as acute and chronic anti-inflammatory effects, with marked activity in the derivates labelled with BAQ and 7-CF3-MAQ. After 7 days of treatment, 7-CF3-MAQ did not induce significant hepatotoxicity, gastrotoxicity or nephrotoxicity.Copyright © 2015 Elsevier Ltd. All rights reserved.