Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine

Rommy Teran; Rommel Guevara; Jessica Mora; Lizeth Dobronski; Olalla Barreiro-Costa; Timo Beske; Jorge Pérez-Barrera; Ramiro Araya-Maturana; Patricio Rojas-Silva; Ana Poveda; HEREDIA MOYA, JORGE HUMBERTO

doi:10.3390/molecules24152696

Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine

Journal

Molecules

ISSN

1420-3049

Date Issued

2019-07-24

Author(s)

Rommy Teran

Rommel Guevara

Jessica Mora

Lizeth Dobronski

Olalla Barreiro-Costa

Facultad de Ciencias de la Salud Eugenio Espejo

Timo Beske

Jorge Pérez-Barrera

Ramiro Araya-Maturana

Patricio Rojas-Silva

Facultad de Ciencias de la Salud Eugenio Espejo

Ana Poveda

HEREDIA MOYA, JORGE HUMBERTO

Facultad de Ciencias de la Salud Eugenio Espejo

DOI

10.3390/molecules24152696

URL

https://cris.ute.edu.ec/handle/123456789/850

Abstract

Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded.