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

被引:43
|
作者
Teran, Rommy [1 ]
Guevara, Rommel [1 ,2 ]
Mora, Jessica [1 ]
Dobronski, Lizeth [3 ]
Barreiro-Costa, Olalla [3 ,4 ]
Beske, Timo [2 ,5 ]
Perez-Barrera, Jorge [1 ,2 ]
Araya-Maturana, Ramiro [6 ]
Rojas-Silva, Patricio [3 ,4 ]
Poveda, Ana [1 ,2 ]
Heredia-Moya, Jorge [3 ,4 ]
机构
[1] Univ Cent Ecuador, Fac Ciencias Quim, Quito 170521, Ecuador
[2] Univ Cent Ecuador, CIZ, Inst Invest Salud Publ & Zoonosis, Quito 170521, Ecuador
[3] Univ Las Amer, Ctr Invest Traslac, Quito 170503, Ecuador
[4] Univ UTE, Fac Ciencias Salud Eugenio Espejo, Ctr Invest Biomed CENBIO, Quito 170527, Ecuador
[5] Univ Cent Ecuador, Fac Med Vet, Quito 170521, Ecuador
[6] Univ Talca, Inst Quim Recursos Nat, PIA CG, Talca 3460000, Chile
来源
MOLECULES | 2019年 / 24卷 / 15期
关键词
schiff base synthesis; Leishmania; antimicrobial activity; cytotoxicity; SPECTRAL CHARACTERIZATION; DNA-BINDING; COMPLEXES; CHEMISTRY; GLYCOXIDATION; INHIBITION; RESISTANCE; DISCOVERY; THERAPY; ANALOGS;
D O I
10.3390/molecules24152696
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
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页数:20
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