Synthesis and Biological Evaluation of Some New Rhodanine Analogues as Aldose Reductase Inhibitors (ARIs)

Khan, Nilofar; Gautam, Girendra; Gupta, Arun Kumar

doi:10.22270/jddt.v9i1-s.2284

Cited by 5 publications

(2 citation statements)

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“…reported a series of 5‐arylbenzylidene‐2,4‐dioxathiazolidines were synthesized and biologically assessed for AR inhibitory property and hypoglycaemic activity. Compound 109 showed potent AR inhibition activity with 83.14 % as compared to standard sorbinil 70.2 % and further series were assessed in‐vivo for their hypoglycaemic potential against Wistar rats, electron‐withdrawing group like No 2 and rhodanine at 3‐position of phenyl containing compound 110 shown to induce the greatest reduction in BGL with 131.11±1.59 mg/dL as compared to standard rosiglitazone 135±1.185 mg/dL [120] . Singh V et al.…”

Section: Discussionmentioning

confidence: 99%

“…Compound 109 showed potent AR inhibition activity with 83.14 % as compared to standard sorbinil 70.2 % and further series were assessed in-vivo for their hypoglycaemic potential against Wistar rats, electron-withdrawing group like No 2 and rhodanine at 3-position of phenyl containing compound 110 shown to induce the greatest reduction in BGL with 131.11 � 1.59 mg/dL as compared to standard rosiglitazone 135 � 1.185 mg/dL. [120] Singh V et al reported benzoxazolyl linked rhodanine and their cycle analogues were synthesized and screened for their αamyloglucosidase inhibitory potential activity. Benzoxazole compound 111 exhibited potent α-amyloglucoridase inhibition with IC 50 : 0.24 � 0.01 μM as compared to standard acarbose with IC 50 : 15.01 � 1.09 μM and hydrogen bond formation between carbonyl group of rhodanine and with LYS1460 amino acid in binding pocket.…”

Section: Synthetic Routes For Rhodanine Derivativesmentioning

confidence: 99%

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Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Gharge,

Alegaon

2024

Chemistry & Biodiversity

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The prevalence of diabetes mellitus is on the rise, which demands for the identification of novel antidiabetic drugs. There is a need for safer and more effective alternatives because the therapy methods now available to manage diabetes have limits. Due to their diverse pharmacological characteristics, heterocyclic molecules with nitrogen and Sulfur atoms have become intriguing candidates in medicinal chemistry. These substances have a wide variety of structures that can be customized to target different pathways associated with diabetes and can affect important biological targets involved in glucose homeostasis. This review provides a thorough summary of the most recent studies on heterocyclic analogues of nitrogen and Sulfur as prospective antidiabetic agents. This review examines the variety of their structural forms, their methods of action, and assesses the results of preclinical and clinical investigations on their effectiveness and safety. Additionally, further optimization and development of innovative antidiabetic medications are highlighted, as well as the difficulties and prospects for the future in utilizing the therapeutic potential of these analogues. This study seeks to stimulate additional investigation and cooperation between researchers and medicinal chemists, promoting improvements in the creation of efficient and secure antidiabetic medicines to fulfil the needs in the management of diabetes.

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Section: Discussionmentioning

confidence: 99%

Section: Synthetic Routes For Rhodanine Derivativesmentioning

confidence: 99%

Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Gharge,

Alegaon

2024

Chemistry & Biodiversity

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Rapid and Environmentally‐Friendly Synthesis of Thiazolidinone Analogues in Deep Eutectic Solvent Complemented with Computational Studies

Kumar,

Seboletswe,

Gcabashe

et al. 2024

ChemistryOpen

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A greener, safer, and more efficient methodology for the synthesis of (Z)‐5‐benzylidene‐2‐thioxothiazolidin‐4‐ones (3 a–u) and (Z)‐5‐benzylidenethiazolidine‐2,4‐diones (4 a–i) has been developed. The deep eutectic solvent (DES) ZnCl2/urea used as a greener solvent as well as a catalyst in this study accelerated the condensation of rhodanine and thiazolidine‐2,4‐dione with different aldehydes to afford the target scaffolds in excellent yields (88‐98 %). The reaction methodology adopted offered significant advantages such as mild reaction conditions, functional group tolerance, quick reaction time, column‐free isolation, catalytic recyclability, and applicability to gram‐scale production. Moreover, density function theory calculations were carried out to investigate the global reactivity and stability profiles of these compounds. Finally, the green metrics analysis supported the greener nature of the present methodology.

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Non-acidic bifunctional benzothiazole-based thiazolidinones with antimicrobial and aldose reductase inhibitory activity as a promising therapeutic strategy for sepsis

et al. 2021

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Sepsis is a life-threatening disease that affects millions of people worldwide. Microbial infections that lead to sepsis syndrome are associated with an increased production of inflammatory molecules. Aldose reductase has recently emerged as a molecular target that is involved in various inflammatory diseases, including sepsis. Herein, a series of previously synthesized benzothiazole-based thiazolidinones that exhibited strong antibacterial and antifungal activities has been evaluated for inhibition efficacy against aldose reductase and selectivity toward aldehyde reductase under in vitro conditions. The most promising inhibitor 5 was characterized with IC 50 value of 3.99 μM and a moderate selectivity. Molecular docking simulations revealed the binding mode of compounds at the active site of human aldose reductase. Moreover, owning to the absence of an acidic pharmacophore, good membrane permeation of the novel aldose reductase inhibitors was predicted. Excellent “drug-likeness” was assessed for most of the compounds by applying the criteria of Lipinski’s “rule of five”.

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Synthesis and Biological Evaluation of Some New Rhodanine Analogues as Aldose Reductase Inhibitors (ARIs)

Cited by 5 publications

References 0 publications

Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Rapid and Environmentally‐Friendly Synthesis of Thiazolidinone Analogues in Deep Eutectic Solvent Complemented with Computational Studies

Non-acidic bifunctional benzothiazole-based thiazolidinones with antimicrobial and aldose reductase inhibitory activity as a promising therapeutic strategy for sepsis

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