Biological Role of Chalcones in Medicinal Chemistry

Tekale, Sunil U.; Mashele, Samson Sitheni; Pooe, Ofentse Jacob; Thore, Shivaji N.; Kendrekar, Pravin

doi:10.5772/intechopen.91626

Cited by 30 publications

(11 citation statements)

References 69 publications

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“…Additionally, chalcones often precipitate in alcohols so their purification is often reduced to a simple filtration and washing with water. Chalcones also exhibit biological activities such as antioxidant, antimicrobial, antifungal, antitumor, anticancer, antimalarial, anti-inflammatory, and antidepressant [251][252][253][254][255]. In 2020, a series of furane-based chalcones CHC-13-CHC-17 was proposed by Lalevée and coworkers (See Figure 13) [143].…”

Section: Chalconesmentioning

confidence: 99%

Recent Advances on Furan-Based Visible Light Photoinitiators of Polymerization

Dumur

2023

Catalysts

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Photopolymerization is an active research field enabling to polymerize in greener conditions than that performed with traditional thermal polymerization. At present, a great deal of effort is devoted to developing visible light photoinitiating systems. Indeed, the traditional UV photoinitiating systems are currently the focus of numerous safety concerns so alternatives to UV light are being actively researched. However, visible light photons are less energetic than UV photons so the reactivity of the photoinitiating systems should be improved to address this issue. In this field, furane constitutes an interesting candidate for the design of photocatalysts of polymerization due to its low cost and its easy chemical modification. In this review, an overview concerning the design of furane-based photoinitiators is provided. Comparisons with reference systems are also established to demonstrate evidence of the interest of these photoinitiators in innovative structures.

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Section: Chalconesmentioning

confidence: 99%

Recent Advances on Furan-Based Visible Light Photoinitiators of Polymerization

Dumur

2023

Catalysts

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“…Medicinal plants have been shown to harbour a wide diversity of chemical structures, displaying a wide range of potency towards M. tuberculosis specificity. [52][53][54][55] Plant-derived compounds with low toxicity and high activity towards M. tuberculosis have previously been identified against M. tuberculosis species and these should be tested in combination with the current first-line drugs. In the last decade, 25 newly approved drugs were derived from natural products, with 31 additional drugs either at or past Phase III clinical trials.…”

Section: Multi-targeting Potential Of Natural Products In Tuberculosis Treatmentmentioning

confidence: 99%

<p>Potential Impact of the Multi-Target Drug Approach in the Treatment of Some Complex Diseases</p>

Makhoba¹,

Viegas²,

Mosa³

et al. 2020

DDDT

148

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It is essential to acknowledge the efforts made thus far to manage or eliminate various disease burden faced by humankind. However, the rising global trends of the so-called incurable diseases continue to put pressure on Pharma industries and other drug discovery platforms. In the past, drugs with more than one target were deemed as undesirable options with interest being on the one-drug-single target. Despite the successes of the single-target drugs, it is currently beyond doubt that these drugs have limited efficacy against complex diseases in which the pathogenesis is dependent on a set of biochemical events and several bioreceptors operating concomitantly. Different approaches have thus been proposed to come up with effective drugs to combat even the complex diseases. In the past, the focus was on producing drugs from screening plant compounds; today, we talk about combination therapy and multi-targeting drugs. The multi-target drugs have recently attracted much attention as promising tools to fight against most challenging diseases, and thus a new research focus area. This review will discuss the potential impact of multi-target drug approach on various complex diseases with focus on malaria, tuberculosis (TB), diabetes and neurodegenerative diseases as the main representatives of multifactorial diseases. We will also discuss alternative ideas to solve the current problems bearing in mind the fourth industrial revolution on drug discovery.

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“…The chemistry of chalcones is a fascinating subject for modern chemical researchers as these structures have many replaceable hydrogens, allowing them to attain a vast number of derived compounds. − This, combined with their Michael acceptor nature, allows a wide variety of therapeutic activities for this family of products. This compound has been reported to have antiallergic, antiobesity, antiparasitic, antioxidant, and neuroprotective activity, among others. − Likewise, benzodihydrofurans, and benzofurans in general, are highly bioactive types of heterocyclic compounds, and they can be found in multiple natural products with pharmacologically relevant properties, including antibacterial, antifungal, analgesic, anti-inflammatory, anticonvulsant, among many others. − Nevertheless, for the past few years, the most appealing property of these scaffolds has been undoubtedly their neuroprotective activity and, consequently, their potential use in the treatment of neurodegenerative conditions like AD. − Regarding this disorder, different types of benzodihydrofurans have been reported as inhibitors of Aβ aggregation process by binding to Aβ peptide. , …”

Section: Introductionmentioning

confidence: 99%

New Benzodihydrofuran Derivatives Alter the Amyloid β Peptide Aggregation: Strategies To Develop New Anti-Alzheimer Drugs

Sánchez

Castillo

Fuentealba

et al. 2023

ACS Chem. Neurosci.

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Alzheimer’s disease is a neurodegenerative disorder that is the leading cause of dementia in elderly patients. Amyloid-β peptide (1–42 oligomers) has been identified as a neurotoxic factor, triggering many neuropathologic events. In this study, 15 chalcones were synthesized employing the Claisen–Schmidt condensation reaction, starting from a compound derived from fomannoxine, a natural benzodihydrofuran whose neuroprotective activity has been proven and reported, and methyl aromatic ketones with diverse patterns of halogenated substitution. As a result, chalcones were obtained, with good to excellent reaction yields from 50 to 98%. Cytotoxicity of the compounds was assessed, and their cytoprotective effect against the toxicity associated with Aβ was evaluated on PC-12 cells. Out of the 15 chalcones obtained, only the 4-bromo substituted was cytotoxic at most tested concentrations. Three synthesized chalcones showed a cytoprotective effect against Aβ toxicity (over 37%). The 2,4,5-trifluoro substituted chalcone was the most promising series since it showed a cytoprotective impact with more than 60 ± 5% of recovery of cellular viability; however, 3-fluoro substituted compound also exhibited important values of recovery (50 ± 6%). The fluorine substitution pattern was shown to be more effective for cytoprotective activity. Specifically, substitution with fluorine in the 3,5-positions turned out to be particularly effective for cytoprotection. Furthermore, fluorinated compounds inhibited the aggregation rate of Aβ, suggesting a dual effect that can be the starting point of new molecules with therapeutic potential.

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Biological Role of Chalcones in Medicinal Chemistry

Cited by 30 publications

References 69 publications

Recent Advances on Furan-Based Visible Light Photoinitiators of Polymerization

Recent Advances on Furan-Based Visible Light Photoinitiators of Polymerization

<p>Potential Impact of the Multi-Target Drug Approach in the Treatment of Some Complex Diseases</p>

New Benzodihydrofuran Derivatives Alter the Amyloid β Peptide Aggregation: Strategies To Develop New Anti-Alzheimer Drugs

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