Overview on Synthesis, Reactions, Applications, and Biological Activities of Schiff Bases

Mukhtar, Shorouk S.; Hassan, Ashraf S.; Morsy, Nesrin M.; Hafez, T. S.; Hassaneen, Hamdi M.; Saleh, Fatma M.

doi:10.21608/ejchem.2021.79736.3920

Cited by 13 publications

(8 citation statements)

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“…Schiff bases are well known for their various biological effects [9], and numerous studies have established this [10][11][12][13]. In 2024, Çavuş et al prepared carbohydrazide-based Schiff base A, which exhibits an antibacterial effect against Bacillus cereus, interacts with plasmid DNA, and has cytotoxic effects on HT-29 cell lines [14].…”

Section: Introductionmentioning

confidence: 99%

Exploring the Potential Biological Activities of Pyrazole-Based Schiff Bases as Anti-Diabetic, Anti-Alzheimer’s, Anti-Inflammatory, and Cytotoxic Agents: In Vitro Studies with Computational Predictions

Naglah,

Almehizia,

Al-Wasidi

et al. 2024

Pharmaceuticals

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In this innovative research, we aim to reveal pyrazole-based Schiff bases as new multi-target agents. In this context, we re-synthesized three sets of pyrazole-based Schiff bases, 5a–f, 6a–f, and 7a–f, to evaluate their biological applications. The data from in vitro biological assays (including antioxidant and scavenging activities, anti-diabetes, anti-Alzheimer’s, and anti-inflammatory properties) of the pyrazole-based Schiff bases 5a–f, 6a–f, and 7a–f showed that the six pyrazole-based Schiff bases 5a, 5d, 5e, 5f, 7a, and 7f possess the highest biological properties among the compounds evaluated. The cytotoxicity against lung (A549) and colon (Caco-2) human cancer types, as well as normal lung (WI-38) cell lines, was evaluated. The data from the cytotoxicity investigation demonstrated that the three Schiff bases 5d, 5e, and 7a are active against lung (A549) cells, while the two Schiff bases 5e and 7a exhibited the highest cytotoxicity towards colon (Caco-2) cells. Additionally, the enzymatic activities against caspase-3 and Bcl-2 of the six pyrazole-based Schiff bases 5a, 5d, 5e, 5f, 7a, and 7f were evaluated. Furthermore, we assessed the in silico absorption, distribution, metabolism, and toxicity (ADMT) properties of the more potent pyrazole-based Schiff bases. After modifying the structures of the six pyrazole-based Schiff bases, we plan to further extend the studies in the future.

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Section: Introductionmentioning

confidence: 99%

Exploring the Potential Biological Activities of Pyrazole-Based Schiff Bases as Anti-Diabetic, Anti-Alzheimer’s, Anti-Inflammatory, and Cytotoxic Agents: In Vitro Studies with Computational Predictions

Naglah,

Almehizia,

Al-Wasidi

et al. 2024

Pharmaceuticals

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“…In view of our previous works (Abd El-All et al, 2016;Ammar et al, 2021;Abdelghany et al, 2021;Elgiushy et al, 2022;Fayed et al, 2021;Hassan, 2021;Hassan et al, 2015Hassan et al, , 2021Hassan et al, , 2022Ibrahim et al, 2021;Mukhtar et al, 2021aMukhtar et al, , 2021bMorsy et al, 2021;Elsherif et al, 2020;Magd-El-Din et al, 2018;Osman et al, 2014) and the abovementioned facts, our work aims to synthesize some of pyrazolo [1,5-a]pyrimidine derivatives 3a-l and 5a-f via the direct cyclo-condensation reaction. Then, the new pyrazolopyrimidine structures were confirmed.…”

Section: Introductionmentioning

confidence: 99%

In vitro enzymatic evaluation of some pyrazolo[1,5‐a]pyrimidine derivatives: Design, synthesis, antioxidant, anti‐diabetic, anti‐Alzheimer, and anti‐arthritic activities with molecular modeling simulation

Hassan

Morsy

Aboulthana

2022

Drug Development Research

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The strategy of utilizing nitrogen compounds in various biological applications has recently emerged as a powerful approach to exploring novel classes of therapeutics to face the challenge of diseases. A series of pyrazolo[1,5‐a]pyrimidine‐based compounds 3a–l and 5a–f were prepared by the direct cyclo‐condensation reaction of 5‐amino‐1H‐pyrazoles 1a, b with 2‐(arylidene)malononitriles and 3‐(dimethylamino)‐1‐aryl‐prop‐2‐en‐1‐ones, respectively. The structures of the new pyrazolo[1,5‐a]pyrimidine compounds were confirmed via spectroscopic techniques. The in vitro biological activities of all pyrazolo[1,5‐a]pyrimidines 3a–l and 5a–f were evaluated by assaying total antioxidant capacity, iron‐reducing power, the scavenging activity against 1‐diphenyl‐2‐picryl‐hydrazyl (DPPH) and 2, 2'‐azinobis‐(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS) radicals, anti‐diabetic, anti‐Alzheimer, and anti‐arthritic biological activities. All compounds displayed good to potent bioactivity, and three compounds 3g, 3h, and 3l displayed the most active derivatives. Among these derivatives, compound 3l exhibited the highest antioxidant (total antioxidant capacity [TAC] = 83.09 mg gallic acid/g; iron‐reducing power [IRP] = 47.93 µg/ml) and free radicals scavenging activities with (DPPH = 18.77 µg/ml; ABTS = 40.44%) compared with ascorbic acid (DPPH = 4.28 µg/ml; ABTS = 38.84%). Furthermore, compound 3l demonstrated the strongest inhibition of α‐amylase with a percent inhibition of 72.91 ± 0.14 compared to acarbose = 67.92 ± 0.09%. Similarly, it displayed acetylcholinesterase inhibition of 62.80 ± 0.06%. However, compound 3i showed a significantly higher inhibition percentage for protein denaturation and proteinase at 20.66 ± 0.00 and 26.42 ± 0.06%, respectively. Additionally, some in silico ADMET properties were predicted and studied. Finally, molecular docking simulation was performed inside the active site of α‐amylase and acetylcholinesterase to study their interactions.

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“…SBs are versatile organic compounds deriving from the condensation of primary amines with carbonyl compounds; they contain an imine group (azomethine, >C=N–). In addition to their usefulness in catalysis [ 1 ], they showed diverse biological activities [ 2 , 3 ] including antimicrobial [ 4 ], antiproliferative [ 5 ], antimalarial [ 6 , 7 ], analgesic, anxiolytic [ 8 ], antidepressant [ 9 ], anti-inflammatory [ 10 , 11 ], antiviral [ 12 ], antipyretic, antibacterial [ 13 ] and antifungal [ 14 ]. Moreover, several studies on SBs-metal complexes showed their use as anti-Alzheimer agents [ 15 , 16 , 17 ], and their potential in the management of diabetes mellitus [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Metal Complexes with Schiff Bases: Data Collection and Recent Studies on Biological Activities

Sinicropi

Ceramella

Iacopetta

et al. 2022

IJMS

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Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significant activities. Schiff bases (SBs) are multifaceted pharmacophores capable of forming chelating complexes with various metals in different oxidation states. Complexes with SBs are extensively studied for their numerous advantages, including low cost and simple synthetic strategies. They have been reported to possess a variety of biological activities, including antimicrobial, anticancer, antioxidant, antimalarial, analgesic, antiviral, antipyretic, and antidiabetic ones. This review summarizes the most recent studies on the antimicrobial and antiproliferative activities of SBs-metal complexes. Moreover, recent studies regarding mononuclear and binuclear complexes with SBs are described, including antioxidant, antidiabetic, antimalarial, antileishmanial, anti-Alzheimer, and catecholase activities.

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Overview on Synthesis, Reactions, Applications, and Biological Activities of Schiff Bases

Cited by 13 publications

References 0 publications

Exploring the Potential Biological Activities of Pyrazole-Based Schiff Bases as Anti-Diabetic, Anti-Alzheimer’s, Anti-Inflammatory, and Cytotoxic Agents: In Vitro Studies with Computational Predictions

Exploring the Potential Biological Activities of Pyrazole-Based Schiff Bases as Anti-Diabetic, Anti-Alzheimer’s, Anti-Inflammatory, and Cytotoxic Agents: In Vitro Studies with Computational Predictions

In vitro enzymatic evaluation of some pyrazolo[1,5‐a]pyrimidine derivatives: Design, synthesis, antioxidant, anti‐diabetic, anti‐Alzheimer, and anti‐arthritic activities with molecular modeling simulation

Metal Complexes with Schiff Bases: Data Collection and Recent Studies on Biological Activities

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