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

被引：20

作者：

Santos, Raquel de Meneses ^{[1
]}

Barros, Pooline Rocha ^{[1
]}

Bortoluzzi, Janaina Heberle ^{[1
]}

Meneghetti, Mario Roberto ^{[1
]}

Cupertino da Silva, Yolanda Karla ^{[2
]}

da Silva, Amanda Evelyn ^{[2
]}

Santos, Mariana da Silva ^{[2
]}

Alexandre-Moreira, Magna Suzana ^{[2
]}

机构：

[1] Univ Fed Alagoas, Inst Quim Biotecnol, GCaR Grp Catalise & Reatividade Quim, Maceio, AL, Brazil

[2] Univ Fed Alagoas, Inst Ciencias Biol & Saude, LaFI, Maceio, AL, Brazil

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 15期

关键词：

Aminoquinolines; Anti-inflammatory; Anti-nociceptive; Rheumatism; Toxicity; ADJUVANT-INDUCED ARTHRITIS; FORMALIN TEST; RATS; INFLAMMATION; CHLOROQUINE; ZYMOSAN; DRUGS; EDEMA; JOINT; MOUSE;

D O I：

10.1016/j.bmc.2015.06.029

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4390 / 4396

页数：7

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