C-cinnamoyl glycosides as a new class of anti-filarial agents

被引：13

作者：

Roy, Priya ^{[3
]}

Dhara, Debashis ^{[1
]}

Parida, Pravat Kumar ^{[1
]}

Kar, Rajiv Kumar ^{[2
]}

Bhunia, Anirban ^{[2
]}

Jana, Kuladip ^{[1
]}

Babu, Santi P. Sinha ^{[3
]}

Misra, Anup Kumar ^{[1
]}

机构：

[1] Bose Inst, Div Mol Med, P-1-12,CIT Scheme 7-M, Kolkata 700054, India

[2] Bose Inst, Dept Biophys, P-1-12,CIT Scheme 7-M, Kolkata 700054, India

[3] Visva Bharati Univ, Parasitol Lab, Dept Zool, Ctr Adv Studies, Santini Ketan 731235, W Bengal, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 114卷

关键词：

C-glycosides; Anti-filarial; Wuchereria bancrofti; Setaria cervi; Aldol reaction; MTT reduction assay; QSAR; ANTIFILARIAL ACTIVITY; LYMPHATIC FILARIASIS; SELECTIVE INHIBITORS; APOPTOSIS; PARASITE; KETONES; IDENTIFICATION; MICROFILARIAE; DISEASE; PHASE;

D O I：

10.1016/j.ejmech.2016.03.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of C-cinnamoyl glycosides has been synthesized in good yield by the BF3 center dot OEt2 catalyzed aldol condensation of C-glycosylated acetone derivative with a variety of aromatic aldehydes. The synthesized compounds were evaluated for their potential as anti-filarial agents against bovine filarial parasite Setaria cervi and human filariid Wuchereria bancrofti using a number of biological assays such as relative movability (RM) assessment and MTT reduction assay. Among twenty seven test compounds six compounds were found active in terms of MIC, IC50 and LC50 values. Further biological studies were carried out using three lead compounds because of their significantly low MIC values and IC50 values compared to the standard anti-filarial drug Ivermectin. In addition, structure activity relationship study of the test compounds has been carried out using 3D-QSAR analysis. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：308 / 317

页数：10

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