Aminonaphthoquinone Mannich Bases Derived from Lawsone and Their Copper(II) Complex Derivatives: Synthesis and Potential Cholinesterase Inhibitors as Identified by On-flow Assay

Vilela, Adriana Ferreira Lopes; Frugeri, Bárbara M.; Sarria, André Lucio Franceschini; Kitamura, Rodrigo Ossamu Saga; Fernandes, João B.; Silva, Maria Fátima das Graças Fernandes da; Cass, Quézia B.; Cardoso, Carmen L.

doi:10.5935/0103-5053.20150281

Cited by 4 publications

(1 citation statement)

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“…Different solid supports can be employed for enzyme immobilization in the development of LC-based on-flow screening assays. Silica-based supports (de Moraes et al, 2012Vanzolini et al, 2013;da Silva et al, 2013;Hu et al, 2015;Silva et al, 2015;Vilela et al, 2015Vilela et al, , 2018Calil et al, 2016;Magalhães et al, 2016;Sarria et al, 2016;Ferreira Lopes Vilela and Cardoso, 2017;Cornelio et al, 2018;Lima et al, 2019;Medina et al, 2019;Qian et al, 2019;Seidl et al, 2019Seidl et al, , 2022Ferey et al, 2019;Chapla et al, 2020;Hou et al, 2020;de Castro et al, 2022) present a versatile and largely explored motif due presence of many hydroxyl groups on its surface. For example, those groups are readily reactive with 3aminopropyltriethoxysilane (APTES), furnishing an amine- rich surface that can further react with glutaraldehyde (GA), yielding a terminal reactive aldehyde surface susceptible reactions with nucleophilic groups present on the enzyme surface (Figure 2B).…”

Section: Solid Supports For Enzyme Immobilization In the Development ...mentioning

confidence: 99%

On-flow enzymatic inhibitor screening: The emerging success of liquid chromatography-based assays

et al. 2022

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Enzymes are targets commonly explored in screening assays aiming to discover new leads in the drug development process. Among the diverse assay models to identify new enzymatic inhibitors, on-flow assays based on liquid chromatography (LC) can be highlighted. In these approaches, the ligand-enzyme interaction can be examined by monitoring the catalytic activity or the affinity/retention. Most applications use the biological target immobilized in solid supports resulting in the acquisition of an immobilized enzymatic reactor (IMER). Coupling IMERs to LC or mass spectrometry (MS) systems allows monitoring enzyme activity online and studying binding events between target and ligands. On-flow screening assays present many advantages for the hit-to-lead process, such as the possibility of system automation, reusability, and high stability. This review covers articles from the last decade that combine the use of varied immobilization methods on different solid supports and several equipment setups in on-flow systems, emphasizing the performance and capacity of recognizing and identifying biologically active compounds in various matrices.

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Section: Solid Supports For Enzyme Immobilization In the Development ...mentioning

confidence: 99%

On-flow enzymatic inhibitor screening: The emerging success of liquid chromatography-based assays

et al. 2022

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Spectroscopic and molecular docking studies on the albumin-binding properties of metal(II) complexes of Mannich base derived from lawsone

Suganthi

Elango

2018

Journal of Biomolecular Structure and Dynamics

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Potential insecticidal activity of aminonaphthoquinone Mannich bases derived from lawsone and their copper (II) complex derivatives

Matos

Volante

Bernardo

et al. 2020

Zeitschrift Für Naturforschung C

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The fall armyworm, Spodoptera frugiperda, is a polyphagous pest that causes important damage in different regions of America and mainly affects corn crops in both tropical and subtropical areas. Currently, control relies on both transgenic plants and/or chemical pesticides. In this work, we describe insecticidal activity against the fall armyworm from a series of Mannich bases (1–10), derived from 2-hydroxy-1,4-naphthoquinone (lawsone), substituted benzaldehydes, and two primary amines, and their Cu2+ complexes (11–20). The [Cu(L)2] complexes were more effective in larval mortality compared to the free Mannich bases. Among the tested compounds, complex 11 showed the highest toxicity, with 70.00% larval mortality.

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Aminonaphthoquinone Mannich Bases Derived from Lawsone and Their Copper(II) Complex Derivatives: Synthesis and Potential Cholinesterase Inhibitors as Identified by On-flow Assay

Cited by 4 publications

References 1 publication

On-flow enzymatic inhibitor screening: The emerging success of liquid chromatography-based assays

On-flow enzymatic inhibitor screening: The emerging success of liquid chromatography-based assays

Spectroscopic and molecular docking studies on the albumin-binding properties of metal(II) complexes of Mannich base derived from lawsone

Potential insecticidal activity of aminonaphthoquinone Mannich bases derived from lawsone and their copper (II) complex derivatives

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