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N-(4-((E)-3-arylacryloyl)phenyl)acetamide derivatives and their antileishmanial activity

Abstract

The antileishmanial activity of a series of enonic derivatives (chalcones) synthesized via Claisen-Schmidt condensation reactions assisted by ultrasonic radiation was characterized by analyzing their cytotoxicity against Leishmania (Viannia) panamensis promastigotes, a species responsible for over 90% of Leishmania cases in Colombia. Two compounds were active against Leishmania with selectivity indexes of LC{sub 50} EC{sub 50} {sup -1} (lethal concentration 50 and effective concentration 50) higher than 27 and 3, respectively. These results suggest that a substitution on one of the two chalcone rings (aromatic ring A) with oxygen is convenient. Compound 3g should be further investigated for its antileishmanial activity, especially for being easy to obtain in high yields, making it possible to produce drugs for the treatment of cutaneous leishmaniasis. (author)
Authors:
Pacheco, Dency J.; Trilleras, Jorge; Prent, Luis; Coaves, Tobinson; [1]  Quiroga, Jairo; [2]  Gutierrez, Jennifer; Delgado, Gabriela; [3]  Marin, Juan C. [4] 
  1. Universidad del Atlantico, Barranquilla-Atlantico (Colombia). Facultad de Ciencias Basicas. Grupo de Investigacion en Compuestos Heterociclicos
  2. Universidad del Valle, Cali (Colombia). Dept. de Quimica. Grupo de Investigacion de Compuestos Heterociclicos
  3. Universidad Nacional de Colombia, Bogota, D.C. (Colombia). Facultad de Ciencias. Departamento de Farmacia. Grupo de Investigacion en Inmunotoxicologia
  4. Universidad Nacional de Colombia, Bogota, D.C. (Colombia). Facultad de Ciencias. Departamento de Farmacia. Grupo de Investigacion Farmacognosia y Fitoquimica
Publication Date:
Oct 15, 2013
Product Type:
Journal Article
Resource Relation:
Journal Name: Journal of the Brazilian Chemical Society; Journal Volume: 24; Journal Issue: 10
Subject:
37 INORGANIC, ORGANIC, PHYSICAL AND ANALYTICAL CHEMISTRY; ACETAMIDE; ACETOPHENONE; CARBON 13; CHEMICAL PREPARATION; ETHANOL; HYDROGEN 1; INFRARED SPECTRA; MASS SPECTRA; METHYLENE CHLORIDE; NMR SPECTRA; PHENYL RADICALS; SILANES
OSTI ID:
22146040
Country of Origin:
Brazil
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0103-5053; CODEN: JOCSET; TRN: BR13V0581100689
Availability:
Available from http://www.scielo.br/pdf/jbchs/v24n10/v24n10a18.pdf
Submitting Site:
BRN
Size:
page(s) 1685-1690
Announcement Date:
Nov 14, 2013

Citation Formats

Pacheco, Dency J., Trilleras, Jorge, Prent, Luis, Coaves, Tobinson, Quiroga, Jairo, Gutierrez, Jennifer, Delgado, Gabriela, and Marin, Juan C. N-(4-((E)-3-arylacryloyl)phenyl)acetamide derivatives and their antileishmanial activity. Brazil: N. p., 2013. Web.
Pacheco, Dency J., Trilleras, Jorge, Prent, Luis, Coaves, Tobinson, Quiroga, Jairo, Gutierrez, Jennifer, Delgado, Gabriela, & Marin, Juan C. N-(4-((E)-3-arylacryloyl)phenyl)acetamide derivatives and their antileishmanial activity. Brazil.
Pacheco, Dency J., Trilleras, Jorge, Prent, Luis, Coaves, Tobinson, Quiroga, Jairo, Gutierrez, Jennifer, Delgado, Gabriela, and Marin, Juan C. 2013. "N-(4-((E)-3-arylacryloyl)phenyl)acetamide derivatives and their antileishmanial activity." Brazil.
@misc{etde_22146040,
title = {N-(4-((E)-3-arylacryloyl)phenyl)acetamide derivatives and their antileishmanial activity}
author = {Pacheco, Dency J., Trilleras, Jorge, Prent, Luis, Coaves, Tobinson, Quiroga, Jairo, Gutierrez, Jennifer, Delgado, Gabriela, and Marin, Juan C.}
abstractNote = {The antileishmanial activity of a series of enonic derivatives (chalcones) synthesized via Claisen-Schmidt condensation reactions assisted by ultrasonic radiation was characterized by analyzing their cytotoxicity against Leishmania (Viannia) panamensis promastigotes, a species responsible for over 90% of Leishmania cases in Colombia. Two compounds were active against Leishmania with selectivity indexes of LC{sub 50} EC{sub 50} {sup -1} (lethal concentration 50 and effective concentration 50) higher than 27 and 3, respectively. These results suggest that a substitution on one of the two chalcone rings (aromatic ring A) with oxygen is convenient. Compound 3g should be further investigated for its antileishmanial activity, especially for being easy to obtain in high yields, making it possible to produce drugs for the treatment of cutaneous leishmaniasis. (author)}
journal = []
issue = {10}
volume = {24}
journal type = {AC}
place = {Brazil}
year = {2013}
month = {Oct}
}