Volume 353, Issue 12 2000157
FULL PAPER

Effect of substituents in the A and B rings of chalcones on antiparasite activity

Luis A. González

Luis A. González

Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia

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Yulieth A. Upegui

Yulieth A. Upegui

Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia

PECET-Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia

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Luis Rivas

Luis Rivas

Grupo de Investigación en Péptidos Antibióticos Eucarióticos, Centro de Investigaciones Biológicas, Madrid, España

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Fernando Echeverri

Fernando Echeverri

Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia

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Gustavo Escobar

Gustavo Escobar

Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia

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Sara M. Robledo

Sara M. Robledo

PECET-Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia

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Wiston Quiñones

Corresponding Author

Wiston Quiñones

Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia

Correspondence Wiston Quiñones, Grupo de Química Orgánica de Productos Naturales, QOPN, Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Calle 70 No. 52–21, A A 1226, Medellín, Colombia.

Email: [email protected]

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First published: 17 August 2020
Citations: 18

Abstract

Chalcones are a group of natural products with many recognized biological activities, including antiparasitic activity. Although a lot of chalcones have been synthetized and assayed against parasites, the number of structural features known to be involved in this biological property is small. Thus, in the present study, 21 chalcones were synthesized to determine the effect of substituents in the A and B rings on the activity against Leishmania braziliensis, Trypanosoma cruzi, and Plasmodium falciparum. The compounds were active against L. braziliensis in a structure-dependent manner. Only one compound was very active against T. cruzi, but none of them had a significant antiplasmodial activity. The electron-donating substituents in ring B and the hydrogen bonds at C-2′ with carbonyl affect the antiparasitic activity.

CONFLICTS OF INTEREST

The authors declare that there are no conflicts of interest.

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