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

Abstract：

:A series of C-cinnamoyl glycosides has been synthesized in good yield by the BF3·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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Roy P,Dhara D,Parida PK,Kar RK,Bhunia A,Jana K,Sinha Babu SP,Misra AK

doi

10.1016/j.ejmech.2016.03.001

subject

Has Abstract

pub_date

2016-05-23 00:00:00

pages

308-17

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30175-1

journal_volume

114

pub_type

杂志文章

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