Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity

被引：68

作者：

Aguiar, Anna C. C. ^{[1
]}

Murce, Erika ^{[2
]}

Cortopassi, Wilian A. ^{[3
]}

Pimentel, Andre S. ^{[2
]}

Almeida, Maria M. F. S. ^{[4
]}

Barros, Daniele C. S. ^{[4
]}

Guedes, Jessica S. ^{[4
]}

Meneghetti, Mario R. ^{[4
]}

Krettli, Antoniana U. ^{[1
]}

机构：

[1] Ctr Pesquisas Rene Rachou Fiocruz, Lab Malaria, Belo Horizonte, MG, Brazil

[2] Pontifical Catholic Univ Rio de Janeiro, Dept Chem, Rio De Janeiro, Brazil

[3] Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA 94143 USA

[4] Univ Fed Alagoas, Inst Quim & Biotecnol, Maceio, Brazil

来源：

INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE | 2018年 / 8卷 / 03期

基金：

巴西圣保罗研究基金会;

关键词：

Malaria; Chloroquine; Resistance; Drug design; PLASMODIUM-FALCIPARUM; ANTIPLASMODIAL ACTIVITY; LACTATE-DEHYDROGENASE; DRUG; RESISTANCE; HEMATIN; DERIVATIVES; INHIBITION; FERROQUINE; HEME;

D O I：

10.1016/j.ijpddr.2018.10.002

中图分类号：

R38 [医学寄生虫学]; Q [生物科学];

学科分类号：

090105 [作物生产系统与生态工程]; 100103 [病原生物学];

摘要：

In spite of recent efforts to eradicate malaria in the world, this parasitic disease is still considered a major public health problem, with a total of 216 million cases of malaria and 445,000 deaths in 2016. Artemisinin-based combination therapies remain effective in most parts of the world, but recent cases of resistance in Southeast Asia have urged for novel approaches to treat malaria caused by Plasmodium falciparum. In this work, we present chloroquine analogs that exhibited high activity against sensitive and chloroquine-resistant P. falciparum blood parasites and were also active against P. berghei infected mice. Among the compounds tested, DAQ, a chloroquine analog with a more linear side chain, was shown to be the most active in vitro and in vivo, with low cytotoxicity, and therefore may serve as the basis for the development of more effective chloroquine analogs to aid malaria eradication.

引用

页码：459 / 464

页数：6

共 48 条

[1]

A molecular marker of artemisinin-resistant Plasmodium falciparum malaria [J].

Ariey, Frederic ;

Witkowski, Benoit ;

Amaratunga, Chanaki ;

Beghain, Johann ;

Langlois, Anne-Claire ;

Khim, Nimol ;

Kim, Saorin ;

Duru, Valentine ;

Bouchier, Christiane ;

Ma, Laurence ;

Lim, Pharath ;

Leang, Rithea ;

Duong, Socheat ;

Sreng, Sokunthea ;

Suon, Seila ;

Chuor, Char Meng ;

Bout, Denis Mey ;

Menard, Sandie ;

Rogers, William O. ;

Genton, Blaise ;

Fandeur, Thierry ;

Miotto, Olivo ;

Ringwald, Pascal ;

Le Bras, Jacques ;

Berry, Antoine ;

Barale, Jean-Christophe ;

Fairhurst, Rick M. ;

Benoit-Vical, Franoise ;

Mercereau-Puijalon, Odile ;

Menard, Didier .

NATURE, 2014, 505 (7481) :50-+

[2]

In vitro susceptibility to a new antimalarial organometallic analogue, ferroquine, of Plasmodium falciparum isolates from the Haut-Ogooue region of Gabon [J].

Atteke, C ;

Ndong, JMM ;

Aubouy, A ;

Maciejewski, L ;

Brocard, J ;

Lébibi, J ;

Deloron, P .

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2003, 51 (04) :1021-1024

[3]

In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border [J].

Barends, Marion ;

Jaidee, Anchalee ;

Khaohirun, Nopparat ;

Singhasivanon, Pratap ;

Nosten, Francois .

MALARIA JOURNAL, 2007, 6 (1)

[4]

Bray PG, 2005, CURR TOP MICROBIOL, V295, P3

[5]

Antimalarial Activity and Mechanisms of Action of Two Novel 4-Aminoquinolines against Chloroquine-Resistant Parasites [J].

Campos Aguiar, Anna Caroline ;

Santos, Raquel de Meneses ;

Barbosa Figueiredo, Flavio Junior ;

Cortopassi, Wilian Augusto ;

Pimentel, Andre Silva ;

Costa Franca, Tanos Celmar ;

Meneghetti, Mario Roberto ;

Krettli, Antoniana Ursine .

PLOS ONE, 2012, 7 (05)

[6]

Quinine and chloroquine differentially perturb heme monomer-dimer equilibrium [J].

Casabianca, Leah B. ;

An, David ;

Natarajan, Jayakumar K. ;

Alumasa, John N. ;

Roepe, Paul D. ;

Wolf, Christian ;

de Dios, Angel C. .

INORGANIC CHEMISTRY, 2008, 47 (13) :6077-6081

[7]

Insights into the Role of Heme in the Mechanism of Action of Antimalarials [J].

Combrinck, Jill M. ;

Mabotha, Tebogo E. ;

Ncokazi, Kanyile K. ;

Ambele, Melvin A. ;

Taylor, Dale ;

Smith, Peter J. ;

Hoppe, Heinrich C. ;

Egan, Timothy J. .

ACS CHEMICAL BIOLOGY, 2013, 8 (01) :133-137

[8]

Docking Studies on the Binding of Quinoline Derivatives and Hematin to Plasmodium Falciparum Lactate Dehydrogenase [J].

Cortopassi, Wilian A. ;

Oliveira, Aline A. ;

Guimaraes, Ana P. ;

Renno, Magdalena N. ;

Krettli, Antoniana U. ;

Franca, Tanos C. C. .

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2011, 29 (01) :207-218

[9]

Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: Design, construction, characterization, and pharmacology of metaquine [J].

Dascombe, MJ ;

Drew, MGB ;

Morris, H ;

Wilairat, P ;

Auparakkitanon, S ;

Moule, WA ;

Alizadeh-Shekalgourabi, S ;

Evans, PG ;

Lloyd, M ;

Dyas, AM ;

Carr, P ;

Ismail, FMD .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (17) :5423-5436

[10]

Antiplasmodial activity of chloroquine analogs against chloroquine-resistant parasites, docking studies and mechanisms of drug action [J].

de Souza, Nicolli B. ;

Carmo, Arturene M. L. ;

da Silva, Adilson D. ;

Franca, Tanos C. C. ;

Krettli, Antoniana U. .

MALARIA JOURNAL, 2014, 13

← 1 2 3 4 5 →