Chalcone-Based Aryloxypropanolamine as a Potential Antidiabetic and Antidyslipidaemic Agent

Shukla, Pragya; Satyanarayana, Mavurapu; Verma, Prem C.; Tiwari, Jaya; Dwivedi, Atma P.; Srivastava, Rohit; Rehuja, Neha; Srivastava, Swayam Prakash; Gautam, Sudeep; Tamrakar, Akhilesh K.; Dwivedi, Anil Kumar; Kushwaha, Hari Narayan; Gautam, Nagsen; Singh, Shio Kumar; Srivastava, Mukesh; Nath, Chandishwar; Raghubir, Ram; Srivastava, Arvind K.; Pratap, Ramendra

doi:10.18520/cs/v112/i08/1675-1689

Cited by 15 publications

(7 citation statements)

References 26 publications

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“…Several authors have evaluated the antihyperglycemic activity of synthetic chalcones in streptozotocin-induced diabetic rats ( Satyanarayana et al, 2004 ; Shukla et al, 2007 ; Najafian et al, 2010 ; Rawat et al, 2011 ; Mahapatra et al, 2017a ; Sengupta et al, 2017 ; Shukla et al, 2017 ; Tajammal et al, 2017 ; Acharjee et al, 2018 ; Naidu, 2018 ; Raju et al, 2018 ). It was found that these compounds have a moderate to potential ability to reduce blood sugar.…”

Section: Preclinical Pharmacological Activities Of Chalconesmentioning

confidence: 99%

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

et al. 2021

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Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

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Section: Preclinical Pharmacological Activities Of Chalconesmentioning

confidence: 99%

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

et al. 2021

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“…Compound 189 (0.92 µM) is a trihydroxy chalcone that is effective against diabetes as it inhibits AMP-kinase activity [ 243 ]. A chalcone with an aryloxy propylamine unit ( 190 ) has been reported as an effective antidiabetic agent, inhibiting type 2 diabetes in rats [ 244 ]. Compound 191 shows good inhibitory activity against PTP1B [ 245 ].…”

Section: Chalcones For Non-infectious Diseasesmentioning

confidence: 99%

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

et al. 2022

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Chalcones are a class of privileged scaffolds with high medicinal significance due to the presence of an α,β-unsaturated ketone functionality. Numerous functional modifications of chalcones have been reported, along with their pharmacological behavior. The present review aims to summarize the structures from natural sources, synthesis methods, biological characteristics against infectious and non-infectious diseases, and uses of chalcones over the past decade, and their structure–activity relationship studies are detailed in depth. This critical review provides guidelines for the future design and synthesis of various chalcones. In addition, this could be highly supportive for medicinal chemists to develop more promising candidates for various infectious and non-infectious diseases.

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“…Chalcones are important precursors for the natural flavonoid biosynthesis [22] and they are also used in various synthetic manipulations for diverse enzyme targets. The chalcones with varied substitutions at different positions have been explored for combating a wide variety of pathological conditions such as in diabetes, [23–25] cancer, [26–28] inflammation, [29,30] cardiac disorders, [31] malaria, [32] oxidative stress and also active against certain type of infections like viral, bacterial and fungal [33–37] . They also offer a wide spectrum of CNS actions including inhibition of acetylcholinesterase (AChE) and butyrylcholinestrase (BuChE), activity on GABA receptor, anti‐depressant, anxiolytic activity, anti‐Alzheimer properties and monoamine oxidase inhibition [38,39] …”

Section: Synthetic Approaches and Design Aspects Of Various Classes Omentioning

confidence: 99%

An Update of Synthetic Approaches and Structure‐Activity Relationships of Various Classes of Human MAO‐B Inhibitors

2021

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The selective MAO‐B inhibition is greatly influenced by the degradation pathways of various biogenic amines. So the design and development of diverse class of MAO‐B inhibitors are considered as an effective adjuvant therapy of various neurodegenerative disorders. Recent studies documented that introduction of an electron rich linker between two aryl or heteroaryl rings explored as a promising structural framework of the inhibition of MAO‐B. The electrophilicity and flexibility character of the linker can anchor different orientation of binding mode in both entrance and substrate cavity of MAO‐B. The current review focus on the design aspect, synthetic route and structure activity relationships (SARs) various class of selective MAO‐B inhibitors like chalcones, coumarins, chromones, pyrazolines, xanthines, isatins, FDA approved analogs etc.

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Chalcone-Based Aryloxypropanolamine as a Potential Antidiabetic and Antidyslipidaemic Agent

Cited by 15 publications

References 26 publications

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

An Update of Synthetic Approaches and Structure‐Activity Relationships of Various Classes of Human MAO‐B Inhibitors

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