Thiopurine derivatives containing triazole and steroid: Synthesis, antimalarial and antileishmanial activities

被引：47

作者：

Corrales, Roberta C. N. R. ^{[1
]}

de Souza, Nicolli B. ^{[2
]}

Pinheiro, Liliane S. ^{[2
]}

Abramo, Clarice ^{[2
]}

Coimbra, Elaine S. ^{[2
]}

Da Silva, Adilson David ^{[1
]}

机构：

[1] Univ Fed Juiz Fora, Dept Quim, ICE, BR-36036900 Juiz De Fora, Minas Gerais, Brazil

[2] Univ Fed Juiz Fora, Dept Parasitol Microbiol & Imunol, ICB, BR-36036900 Juiz De Fora, Minas Gerais, Brazil

来源：

BIOMEDICINE & PHARMACOTHERAPY | 2011年 / 65卷 / 03期

关键词：

6-thiopurine; 1,2,3-triazole; Click chemistry; Antimalarial and antileishmanial activities; Plasmodium; Leishmania; CHOLIC-ACID DERIVATIVES; PLASMODIUM-FALCIPARUM; BIOLOGICAL EVALUATION; IN-VITRO; 1,2,4-TRIAZOLES; LEISHMANIASIS; CONJUGATE; DESIGN;

D O I：

10.1016/j.biopha.2010.10.013

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

A series of novel 6-thiopurine derivates containing 1,2,3-triazole were synthesized and their in vivo antimalarial activity and in vitro antileishmanial activity were examined. The compounds 10, 11, 12 and 14 presented higher values of inhibition of parasite multiplication than chloroquine. For antileishmanial activity, the compound 14 showed activity against the three species of Leishmania tested. None of compounds showed cytotoxicity against mammalian cells. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：198 / 203

页数：6

共 39 条

[1] Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: Impending synergistic agents [J].

Bavikar, Sudhir N. ;

Salunke, Deepak B. ;

Hazra, Braja G. ;

Pore, Vandana S. ;

Dodd, Robert H. ;

Thierry, Josiane ;

Shirazi, Fazal ;

Deshpande, Mukund V. ;

Kadreppa, Sreenath ;

Chattopadhyay, Samit .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (20) :5512-5517

[2]

Bechet K.H., 1972, DRUGS GERM, V15, P79

[3] Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters [J].

Bhat, L ;

Jandeleit, B ;

Dias, TM ;

Moors, TL ;

Gallop, MA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (01) :85-87

[4]

Bock V.D., 2006, Eur. J. Org. Chem, V51

[5]

Bock VD, 2006, J ORG CHEM, V71, P51

[6] A conditional mutant deficient in hypoxanthine-guanine phosphoribosyltransferase and xanthine phosphoribosyltransferase validates the purine salvage pathway of Leishmania donovani [J].

Boitz, Jan M. ;

Ullman, Buddy .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2006, 281 (23) :16084-16089

[7] Synthesis and biological evaluation of some 6-substituted purines [J].

Braga, Fernanda Gambogi ;

Coimbra, Elaine Soares ;

Matos, Magnum de Oliveira ;

Lino Carmo, Arturene Maria ;

Cancio, Marisa Damato ;

da Silva, Adilson David .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2007, 42 (04) :530-537

[8]

CARVALHO LH, 1991, BRAZ J MED BIOL RES, V24, P1113

[9] Current Treatment and Drug Discovery Against Leishmania spp. and Plasmodium spp.: A Review [J].

Cruz, Angela Kaysel ;

de Toledo, Juliano Simoes ;

Falade, Mofolusho ;

Terrao, Monica Cristina ;

Kamchonwongpaisan, Sumalee ;

Kyle, Dennis E. ;

Uthaipibull, Chairat .

CURRENT DRUG TARGETS, 2009, 10 (03) :178-192

[10] SYNTHESIS AND BIOLOGICAL-ACTIVITY OF METHYL-D-GLUCOPYRANOSIDE DERIVATIVES OF MERCAPTOPURINE AND MERCAPTOPYRIMIDINE [J].

DASILVA, AD ;

MACHADO, AS ;

TEMPETE, C ;

ROBERTGERO, M .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1994, 29 (02) :149-152

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