TY - JOUR
T1 - Characterization of antimicrobial, antioxidant, and leishmanicidal activities of Schiff base derivatives of 4-aminoantipyrine
AU - Teran, Rommy
AU - Guevara, Rommel
AU - Mora, Jessica
AU - Dobronski, Lizeth
AU - Barreiro-Costa, Olalla
AU - Beske, Timo
AU - Pérez-Barrera, Jorge
AU - Araya-Maturana, Ramiro
AU - Rojas-Silva, Patricio
AU - Poveda, Ana
AU - Heredia-Moya, Jorge
N1 - Publisher Copyright:
© 2019 by the authors
PY - 2019/7/24
Y1 - 2019/7/24
N2 - 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.
AB - 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.
KW - Antimicrobial activity
KW - Cytotoxicity
KW - Leishmania
KW - Schiff base synthesis
UR - http://www.scopus.com/inward/record.url?scp=85070069307&partnerID=8YFLogxK
U2 - 10.3390/molecules24152696
DO - 10.3390/molecules24152696
M3 - Artículo
C2 - 31344947
AN - SCOPUS:85070069307
SN - 1420-3049
VL - 24
JO - Molecules
JF - Molecules
IS - 15
M1 - 2696
ER -