Design, synthesis, and molecular docking of cysteine-based sulphonamide derivatives as antimicrobial agents

Egbujor, Melford C.; Okafor, SundayN; Okoro, Uchechukwu C.; Egu, Samuel Attah; Amasiatu, IfeanyiS; Egwuatu, PiusI; Umeh, OderaR; Ibo, EziafakaegoM

doi:10.4103/1735-5362.329930

Cited by 11 publications

(5 citation statements)

References 31 publications

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“…Their usual incorporation into a core ring structure gives them specific conformations which fit the active sites [ 79 ]. Sulfonyl group-containing compounds exhibit therapeutic effects against bacterial infections [ 80 , 81 , 82 , 83 , 84 , 85 , 86 ], tumors [ 87 , 88 ], Alzheimer’s disease [ 89 ], oxidative stress-related diseases [ 90 , 91 , 92 , 93 ], and diabetes [ 79 ]. Moreover, sulfonyl-containing compounds have been found to activate the Nrf2 pathway and inhibit Keap1–Nrf2 protein–protein interaction, thereby alleviating oxidative stress and inflammatory conditions [ 94 ].…”

Section: Nrf2-activating Synthetic Organosulfur Compoundsmentioning

confidence: 99%

The Role of Organosulfur Compounds as Nrf2 Activators and Their Antioxidant Effects

et al. 2022

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Nuclear factor erythroid 2-related factor 2 (Nrf2) signaling has become a key pathway for cellular regulation against oxidative stress and inflammation, and therefore an attractive therapeutic target. Several organosulfur compounds are reportedly activators of the Nrf2 pathway. Organosulfur compounds constitute an important class of therapeutic agents in medicinal chemistry due to their ability to participate in biosynthesis, metabolism, cellular functions, and protection of cells from oxidative damage. Sulfur has distinctive chemical properties such as a large number of oxidation states and versatility of reactions that promote fundamental biological reactions and redox biochemistry. The presence of sulfur is responsible for the peculiar features of organosulfur compounds which have been utilized against oxidative stress-mediated diseases. Nrf2 activation being a key therapeutic strategy for oxidative stress is closely tied to sulfur-based chemistry since the ability of compounds to react with sulfhydryl (-SH) groups is a common property of Nrf2 inducers. Although some individual organosulfur compounds have been reported as Nrf2 activators, there are no papers with a collective analysis of these Nrf2-activating organosulfur compounds which may help to broaden the knowledge of their therapeutic potentials and motivate further research. In line with this fact, for the first time, this review article provides collective and comprehensive information on Nrf2-activating organosulfur compounds and their therapeutic effects against oxidative stress, thereby enriching the chemical and pharmacological diversity of Nrf2 activators.

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Section: Nrf2-activating Synthetic Organosulfur Compoundsmentioning

confidence: 99%

The Role of Organosulfur Compounds as Nrf2 Activators and Their Antioxidant Effects

et al. 2022

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“…This property also makes α,β-unsaturated sulfonyls to act as powerful dienophiles [ 180 ]. Several sulfonyl-containing compounds exhibit significant antioxidant and anti-inflammatory activities [ 181 , 182 , 183 , 184 ]. α,β-unsaturated sulfonyls are notable building blocks in the synthesis of organic compounds [ 185 ].…”

Section: αβ-Unsaturated Sulfonylsmentioning

confidence: 99%

An Overview of NRF2-Activating Compounds Bearing α,β-Unsaturated Moiety and Their Antioxidant Effects

Egbujor

Buttari²,

Profumo³

et al. 2022

IJMS

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The surge of scientific interest in the discovery of Nuclear Factor Erythroid 2 (NFE2)-Related Factor 2 (NRF2)-activating molecules underscores the importance of NRF2 as a therapeutic target especially for oxidative stress. The chemical reactivity and biological activities of several bioactive compounds have been linked to the presence of α,β-unsaturated structural systems. The α,β-unsaturated carbonyl, sulfonyl and sulfinyl functional groups are reportedly the major α,β-unsaturated moieties involved in the activation of the NRF2 signaling pathway. The carbonyl, sulfonyl and sulfinyl groups are generally electron-withdrawing groups, and the presence of the α,β-unsaturated structure qualifies them as suitable electrophiles for Michael addition reaction with nucleophilic thiols of cysteine residues within the proximal negative regulator of NRF2, Kelch-like ECH-associated protein 1 (KEAP1). The physicochemical property such as good lipophilicity of these moieties is also an advantage because it ensures solubility and membrane permeability required for the activation of the cytosolic NRF2/KEAP1 system. This review provides an overview of the reaction mechanism of α,β-unsaturated moiety-bearing compounds with the NRF2/KEAP1 complex, their pharmacological properties, structural activity-relationship and their effect on antioxidant and anti-inflammatory responses. As the first of its kind, this review article offers collective and comprehensive information on NRF2-activators containing α,β-unsaturated moiety with the aim of broadening their therapeutic prospects in a wide range of oxidative stress-related diseases.

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“…Finally, phosphoserine phosphatase (PSPH) breaks down phosphorine to produce serine (Nelson et al 2021 ). Serine exhibits significant antioxidant activities (Maralani et al 2012 ; Egbujor et al 2019 ). (Chen et al 2021 ) reported that serine supplementation could represent a nutritional strategy for improving skeletal muscle functions in doxorubicin-exposed patients.…”

Section: Introductionmentioning

confidence: 99%

An insight into role of amino acids as antioxidants via NRF2 activation

Egbujor,

Olaniyan,

Emeruwa

et al. 2024

Amino Acids

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Oxidative stress can affect the protein, lipids, and DNA of the cells and thus, play a crucial role in several pathophysiological conditions. It has already been established that oxidative stress has a close association with inflammation via nuclear factor erythroid 2-related factor 2 (NRF2) signaling pathway. Amino acids are notably the building block of proteins and constitute the major class of nitrogen-containing natural products of medicinal importance. They exhibit a broad spectrum of biological activities, including the ability to activate NRF2, a transcription factor that regulates endogenous antioxidant responses. Moreover, amino acids may act as synergistic antioxidants as part of our dietary supplementations. This has aroused research interest in the NRF2-inducing activity of amino acids. Interestingly, amino acids' activation of NRF2-Kelch-like ECH-associated protein 1 (KEAP1) signaling pathway exerts therapeutic effects in several diseases. Therefore, the present review will discuss the relationship between different amino acids and activation of NRF2–KEAP1 signaling pathway pinning their anti-inflammatory and antioxidant properties. We also discussed amino acids formulations and their applications as therapeutics. This will broaden the prospect of the therapeutic applications of amino acids in a myriad of inflammation and oxidative stress-related diseases. This will provide an insight for designing and developing new chemical entities as NRF2 activators.

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Design, synthesis, and molecular docking of cysteine-based sulphonamide derivatives as antimicrobial agents

Cited by 11 publications

References 31 publications

The Role of Organosulfur Compounds as Nrf2 Activators and Their Antioxidant Effects

The Role of Organosulfur Compounds as Nrf2 Activators and Their Antioxidant Effects

An Overview of NRF2-Activating Compounds Bearing α,β-Unsaturated Moiety and Their Antioxidant Effects

An insight into role of amino acids as antioxidants via NRF2 activation

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