Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail

被引：97

作者：

Hayat, Faisal ^{[1
]}

Salahuddin, Attar ^{[1
]}

Umar, Sadiq ^{[2
]}

Azam, Amir ^{[1
]}

机构：

[1] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India

[2] Jamia Hamdard, Dept Toxicol, New Delhi 110062, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 10期

关键词：

Pyrazoline derivatives; Entamoeba histolytica; MTT assay; AMEBIC LIVER-ABSCESS; ENTAMOEBA-HISTOLYTICA; METRONIDAZOLE; CHALCONES; DESIGN;

D O I：

10.1016/j.ejmech.2010.07.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cyclization of chalcones (1a-1j) with 2-(quinolin-8-yloxy) acetohydrazide (2) under basic condition led to the formation of new compounds. pyrazoline derivatives (3a-3j) In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica The results showed that the compounds 3d, 3g, 3h, and 3j exhibited promising antiamoebic activity (IC(50) = 0 05 mu M, 0 31 mu M, 006 mu M, 0 29 mu M) respectively than the standard drug metronidazole (IC(50) = 1 84 mu M). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds 3d, 3g, 3h, 3j and metronidazole were nontoxic at the concentration range of 1.56-50 mu M. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：4669 / 4675

页数：7

共 28 条

[1] Successful treatment of metronidazole- and albendazole-resistant giardiasis with nitazoxanide in a patient with acquired immunodeficiency syndrome [J].

Abboud, P ;

Lemée, V ;

Gargala, G ;

Brasseur, P ;

Ballet, JJ ;

Borsa-Lebas, F ;

Caron, F ;

Favennec, L .

CLINICAL INFECTIOUS DISEASES, 2001, 32 (12) :1792-1794

[2] Synthesis and antimicrobial activity of succinimido(2-aryl-4-oxo-3{[( quinolin-8-yloxy)acetyl]amino}-1,3-thiazolidin-5-yl)acetates [J].

Ahmed, Maqbool ;

Sharma, Ranjana ;

Nagda, Devendra P. ;

Jat, Jawahar L. ;

Talesara, Ganpat L. .

ARKIVOC, 2006, :66-75

[3]

Azad Muhammad., 2007, J. of Applied sciences. Vol, V7, P2485

[4] Synthesis and anti-inflammatory activity of 1-acetyl-5-substitute daryl-3-(β-aminonapthyl)-2-pyrazolines and β-(substituted aminoethyl) amidonaphthalenes [J].

Bansal, E ;

Srivastava, VK ;

Kumar, A .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2001, 36 (01) :81-92

[5] Treatment of amoebic liver abscess with metronidazole alone or in combination with ultrasound-guided needle aspiration: a comparative, prospective and randomized study [J].

Blessmann, J ;

Binh, HD ;

Hung, DM ;

Tannich, E ;

Burchard, G .

TROPICAL MEDICINE & INTERNATIONAL HEALTH, 2003, 8 (11) :1030-1034

[6] Longitudinal study of intestinal Entamoeba histolytica infections in asymptomatic adult carriers [J].

Blessmann, J ;

Ali, IKM ;

Nu, PAT ;

Dinh, BT ;

Viet, TQN ;

Le Van, A ;

Clark, CG ;

Tannich, E .

JOURNAL OF CLINICAL MICROBIOLOGY, 2003, 41 (10) :4745-4750

[7] Present trends and future strategy in chemotherapy of malaria [J].

Chauhan, PMS ;

Srivastava, SK .

CURRENT MEDICINAL CHEMISTRY, 2001, 8 (13) :1535-1542

[8] Design, synthesis and evaluation of novel quinolyl chalcones as antibacterial agents [J].

Chikhalia, Kishor H. ;

Patel, Mayank J. ;

Vashi, Dhaval B. .

ARKIVOC, 2008, :189-197

[9] NEW MEDIUM FOR AXENIC CULTIVATION OF ENTAMOEBA-HISTOLYTICA AND OTHER ENTAMOEBA [J].

DIAMOND, LS ;

HARLOW, DR ;

CUNNICK, CC .

TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE, 1978, 72 (04) :431-432

[10] Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities [J].

Dominguez, Jose N. ;

Leon, Caritza ;

Rodrigues, Juan ;

Gamboa de Dominguez, Neira ;

Gut, Jiri ;

Rosenthal, Philip J. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (04) :1457-1462

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