About: Synthesis and In vitro Leishmanicidal Activities of Six Quercetin Derivatives

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An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Synthesis and In vitro Leishmanicidal Activities of Six Quercetin Derivatives
Creator	Ghanadian, Mustafa Mohajeri, Maryam Ostadhusseini, Ehsan Pestechian, Nader Saberi, Sedighe Saghaei, Lotfollah
source	PMC
abstract	BACKGROUND: Today, leishmaniasis is a widespread, infectious parasitic disease caused by Leishmania spp. Natural-derived compounds are likely to provide a valuable source of new pharmaceuticals, and among them, quercetin derivatives may have antileishmanial effects. The antileishmanial activity of 3,5,7,3’,4’-pentahydroxyflavonol (quercetin) derivatives is partly attributed to the position and pKa of phenolic or catechol hydroxyl groups. Therefore, to optimize their leishmanicidal effect, the structural features of quercetin and its derivatives were improved by acylation or alkylation of hydroxyl groups and changing their pKa and consequently their activities. MATERIALS AND METHODS: In this study, during a regioselective method, quercetin derivatives were synthesized. The structures of synthesized compounds were confirmed by mass, IR, (1)H-, and (13)C-NMR spectral data. The antileishmanial activities of compounds 1–6 were compared with glucantime as the standard drug against promastigotes of Leishmania major using standard cell-based leishmanicidal assay. RESULTS: In this study, during a regioselective method, two 7-O-quercetin derivatives (5 and 6), and three quercetin acetate derivatives (2, 3, and 4) were synthesized. In detail, the IC(50) values found against L. major were (1) 2.5 ± 0.92; (2) 2.85 ± 0.99; (3) 15.5 ± 1.95; (4) 13.5 ± 3.5; (5) 2.6 ± 0.57; and (6) 1.3 ± 0.35 μM while IC(50) value of glucantime as the standard drug was 88.5 ± 9.47 μM. CONCLUSIONS: The present study showed an effective antileishmanial activity of quercetin semisynthetic compounds (1–6) against in vitro promastigotes of L. major. Among them, quercetin analogs with more lipophilic and iron-chelating activity showed more antiparasite activity.
has issue date	2018-04-24(xsd:dateTime)
bibo:doi	10.4103/abr.abr_76_17
bibo:pmid	29862213
has license	cc-by-nc-sa
schema:url	https://doi.org/10.4103/abr.abr_76_17
resource representing a document's title	Synthesis and In vitro Leishmanicidal Activities of Six Quercetin Derivatives
has PubMed Central identifier	PMC5952540
has PubMed identifier	29862213
schema:publication	Adv Biomed Res
resource representing a document's body	covid:PMC5952540#body_text
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