1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

被引：67

作者：

Kumar, Kewal ^{[1
]}

Pradines, Bruno ^{[2
,3
,4
]}

Madamet, Marilyn ^{[3
,4
,5
]}

Amalvict, Remy ^{[3
,4
,5
]}

Benoit, Nicolas ^{[3
,4
,5
]}

Kumar, Vipan ^{[1
]}

机构：

[1] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India

[2] Inst Rech Biomed Armees, Dept Malad Infect, Unite Parasitol & Entomol, Bretigny Sur Orge, France

[3] Aix Marseille Univ, Unite Rech Malad Infect & Trop Emergentes, Inserm 1095, UM 63,CNRS 7278,IRD 198, Marseille, France

[4] Ctr Natl Reference Paludisme, Marseille, France

[5] Hop Instruct Armees Laveran, Equipe Residente Rech Infectiol Trop, Inst Rech Biomed Armees, Marseille, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 87卷

关键词：

Isatin-ferrocene conjugates; Click chemistry; Structure activity relationship; Antimalarial evaluation; Cytotoxicity; PLASMODIUM-FALCIPARUM; CYTOTOXIC EVALUATION; CLICK CHEMISTRY; MEDICINAL CHEMISTRY; GENETIC DIVERSITY; CHEMICAL-BIOLOGY; INHIBITORS; OXINDOLES; DERIVATIVES; FERROQUINE;

D O I：

10.1016/j.ejmech.2014.10.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their anti-plasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC50 values of 3.76 and 4.58 mu M against 3D7 and W2 strains, respectively. (c) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：801 / 804

页数：4

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