Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines

被引：141

作者：

Acharya, Badri Narayan ^{[1
]}

Saraswat, Deepika ^{[1
]}

Tiwari, Mugdha ^{[1
]}

Shrivastava, Asish Kumar ^{[1
]}

Ghorpade, Ramarao ^{[1
]}

Bapna, Saroj ^{[2
]}

Kaushik, Mahabir Parshad ^{[1
]}

机构：

[1] Def Res & Dev Estab, Gwalior 474002, India

[2] Hafkine Inst Training Res & Testing, Bombay 400012, Maharashtra, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 02期

关键词：

Pyrazoline; Plasmodium falciparum; Haem detoxification; Antimalarial; HEME POLYMERIZATION; MONOAMINE-OXIDASE; IN-VITRO; INHIBITION; MALARIA; DERIVATIVES; BINDING; DESIGN;

D O I：

10.1016/j.ejmech.2009.10.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,3,5-trisubstituted pyrazolines were synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive (MRC-02) as well as chloroquine resistant (RKL9) strains of Plasmodium falciparum. The activity was at nano molar concentration. beta-hematin formation inhibition activity (BHIA(50)) of the pyrazolines were determined and correlated with antimalarial activity. A reasonably good correlation (r = 0.62) was observed between antimalarial activity (IC50) and BHIA(50). This suggests that antimalarial mode of action of this class of compounds appears to be similar to that of chloroquine and involves the inhibition of hemozoin formation. Some of the compounds were showing better antimalarial activity than chloroquine against resistant strain of P. falciparum and were also found active in the in vivo experiment. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：430 / 438

页数：9

共 38 条

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