title: 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.
authors.affiliation: Parasitology Laboratory, Department of Zoology (Centre for Advanced Studies), Visva-Bharati University, Santiniketan 731235, West Bengal, India.
authors.forename: Priya
authors.initials: P
authors.lastname: Roy
authors.affiliation: Bose Institute, Division of Molecular Medicine, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India.
authors.forename: Debashis
authors.initials: D
authors.lastname: Dhara
authors.affiliation: Bose Institute, Division of Molecular Medicine, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India.
authors.forename: Pravat Kumar
authors.initials: PK
authors.lastname: Parida
authors.affiliation: Bose Institute, Department of Biophysics, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India.
authors.forename: Rajiv Kumar
authors.initials: RK
authors.lastname: Kar
authors.affiliation: Bose Institute, Department of Biophysics, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India.
authors.forename: Anirban
authors.initials: A
authors.lastname: Bhunia
authors.affiliation: Bose Institute, Division of Molecular Medicine, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India. Electronic address: kuladip@jcbose.ac.in.
authors.forename: Kuladip
authors.initials: K
authors.lastname: Jana
authors.affiliation: Parasitology Laboratory, Department of Zoology (Centre for Advanced Studies), Visva-Bharati University, Santiniketan 731235, West Bengal, India. Electronic address: spsinhababu@gmail.com.
authors.forename: Santi P
authors.initials: SP
authors.lastname: Sinha Babu
authors.affiliation: Bose Institute, Division of Molecular Medicine, P-1/12, C.I.T. Scheme VII-M, Kolkata 700054, India. Electronic address: akmisra69@gmail.com.
authors.forename: Anup Kumar
authors.initials: AK
authors.lastname: Misra
mesh_terms: D000818:Animals; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D005368:Filariasis / Q000188:drug therapy*; D005370:Filarioidea / Q000187:drug effects*; D006027:Glycosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D021281:Quantitative Structure-Activity Relationship
chemical_list: D006027:Glycosides
keywords: Aldol reaction; Anti-filarial; C-glycosides; MTT reduction assay; QSAR; Setaria cervi; Wuchereria bancrofti