Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

Keri, Rangappa S.; Budagumpi, Srinivasa; Somappa, Sasidhar B.

doi:10.1111/jcpt.13644

Cited by 35 publications

(15 citation statements)

References 112 publications

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“…The diverse array of biological characteristics ( Srikrishna et al, 2018 ) has rendered this notable category of heterocyclic compounds appealing to medicinal chemists throughout the years. These properties encompass antioxidant ( Stanchev et al, 2009 ), anticonvulsant ( Keri et al, 2022 ), antitumor ( Wu et al, 2020 ), anti-inflammatory ( Grover and Jachak, 2015 ), and antimicrobial ( Al-Majedy et al, 2017 ) activities. Several coumarin derivatives have been approved by FDA for clinical usage.…”

Section: Introductionmentioning

confidence: 99%

Syntheses, reactivity, and biological applications of coumarins

Citarella,

Vittorio,

Dank

et al. 2024

Front. Chem.

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This comprehensive review, covering 2021–2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis and functionalization of coumarins have advanced with innovative strategies. This enabled the incorporation of diverse functional fragments or the construction of supplementary cyclic architectures, thereby the biological and physico-chemical properties of the compounds obtained were enhanced. The unique chemical structure of coumarine facilitates binding to various targets through hydrophobic interactions pi-stacking, hydrogen bonding, and dipole-dipole interactions. Therefore, this important scaffold exhibits promising applications in uncountable fields of medicinal chemistry (e.g., neurodegenerative diseases, cancer, inflammation).

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Section: Introductionmentioning

confidence: 99%

Syntheses, reactivity, and biological applications of coumarins

Citarella,

Vittorio,

Dank

et al. 2024

Front. Chem.

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“…16,17 In addition, coumarins showed broad pharmacological activities. 18,19 Coumarins and their derivatives demonstrated various therapeutic properties including antioxidant, 20 antiinflammatory, 21 anticancer, 22 anti-diabetic 23 and anti-obesity. 24 These talented findings provoked us to evaluate the anti-obesity activity of the coumarin glucoside, namely Cichorioside (cichoriin).…”

Section: Introductionmentioning

confidence: 99%

Cichorioside a biocoumarin modulates lipid and glucose storage on 3T3-L1 cell lines: In vitro and in silico approach

Alqahtani¹,

Alsuliman²,

Alasoom³

et al. 2023

Pharmacogn J.

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Natural coumarins are reputed to demonstrate several biological effects to improve adverse health conditions including; obesity. This study was conducted to explore the potential in vitro lipid and glucose modulatory activity of cichorioside on 3T3-L1 cell lines . Methods: The 3T3-L1 cell lines were cultured and cell viability was assessed. Glucose content in medium of cultured cells was measured. Differentiation of 3T3-L1 cells from pre-adipocytes to adipocytes was evaluated upon addition of cichorioside. Expression of mRNA of the peroxisome proliferator-activated receptor gamma (PPARγ) was estimated. Results: Survival of around 90% of cultured cells was observed at 10μM cichorioside. Cichorioside inhibited glucose uptake from the medium by the 3T3-L1 cell lines. Cichorioside considerably inhibited pre-adipocyte differentiation and the lipid content in intercellular storage. Cichorioside demonstrated an upregulation of the mRNA expression of PPARγ. Moreover, the docking studies supported the results via the deep interaction of cichorioside with amino acids residue of PPAR-γ. Taken together, these findings are the first report on in vitro evaluation of cichorioside to modulate the lipid storage and glucose uptake of cultured 3T3-L1 cell lines.

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“…Condensed heterocyclic systems containing both furan and pyrone fragments are presented in various biologically active compounds and natural products [1][2][3][4][5][6][7][8][9]. Among the considered classes of heterocycles 2H-furo [3,2-b]pyran-2-one and their fused analogs are almost not studied.…”

Section: Introductionmentioning

confidence: 99%

Straightforward method for the synthesis of 2H‐furo[3,2‐b]pyran‐2‐one derivatives starting from allomaltol

Komogortsev,

Lichitsky,

Milyutin

et al. 2023

Journal of Heterocyclic Chem

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We developed a facile approach for the preparation of a rare 2H‐furo[3,2‐b]pyran‐2‐one system. The suggested method is based on a two‐step process using unsubstituted allomaltol as a starting compound. The key stage of the considered route is a condensation of 2‐(2‐aryl‐2‐oxoethyl)‐3‐hydroxy‐6‐methyl‐4H‐pyran‐4‐ones with 1,1‐carbonyldiimidazole. The advantages of the presented method are commercially available starting materials and convenient experimental procedures including simple isolation of the target compounds. The structure of one of the 2H‐furo[3,2‐b]pyran‐2‐ones was confirmed by x‐ray diffraction.

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Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

Cited by 35 publications

References 112 publications

Syntheses, reactivity, and biological applications of coumarins

Syntheses, reactivity, and biological applications of coumarins

Cichorioside a biocoumarin modulates lipid and glucose storage on 3T3-L1 cell lines: In vitro and in silico approach

Straightforward method for the synthesis of 2H‐furo[3,2‐b]pyran‐2‐one derivatives starting from allomaltol

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