In vitro studies of potent aldose reductase inhibitors: Synthesis, characterization, biological evaluation and docking analysis of rhodanine-3-hippuric acid derivatives

2020 ◽  
Vol 97 ◽  
pp. 103640 ◽  
Author(s):  
Stephen Kumar Celestina ◽  
Kaveri Sundaram ◽  
Subban Ravi
Keyword(s):  
Aldose Reductase ◽  
Hippuric Acid ◽  
Biological Evaluation ◽  
In Vitro Studies ◽  
Docking Analysis ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

In-vitro Studies on α-Amylase, α-Glucosidase and Aldose Reductase Inhibitors found in Endophytic Fungi Isolated from Ocimum sanctum

2015 ◽  
Vol 10 (2) ◽  
pp. 129-136
Author(s):  
Pavithra N. ◽  
Sathish L. ◽  
Suneel Kumar A. ◽  
Venkatarathanamma V. ◽  
Pushpalatha H. ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Endophytic Fungi ◽  
In Vitro Studies ◽  
Ocimum Sanctum ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

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

2019 ◽  
Vol 9 (1-s) ◽  
pp. 161-167
Author(s):  
Neelam Khan ◽  
Girendra Gautam ◽  
Arun K. Gupta
Keyword(s):  
Diabetes Mellitus ◽  
Aldose Reductase ◽  
Polyol Pathway ◽  
Biological Evaluation ◽  
Drug Candidates ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Secondary Complication

Diabetes mellitus is a metabolic disorder characterized by hyperglycemia resulting long-term secondary complication. Aldose reductase, the rate-limiting enzyme of the polyol pathway, plays a key role in the treatment of diabetic complications. Appropriately, inhibition of this enzyme is emerging as a major therapeutic strategy for the pathogenesis of secondary complication. In this study, we describe a series of 5 aryl benzylidene -thiazolidine, 4-dione derivatives, F3 synthesized as aldose reductase inhibitors. Besides inhibiting efficiently the target enzyme, F4 and F5 showed additional AR inhibitory as well as hypoglycaemic activity (146.15 and 175.20 mg/dl ) thus emerging as novel dual acting compounds. The bezylidene derivative F3, the most promising of the whole series, showed a well-balanced, consisting of ALR2 inhibitory efficacy (83.00% at 10µg/mL), similarly, F3 have lower blood glucose level in the range of 131.11 mg/dl at 15 mg/kg body weight. This compound show robust in vitro and in vivo efficacy, and could be considered as promising dual target antidiabetic drug candidates. Keywords: Diabetes mellitus, hyperglycemia, Aldose reductase inhibitors

scholarly journals Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2867
Author(s):  
Lucia Kovacikova ◽  
Marta Soltesova Prnova ◽  
Magdalena Majekova ◽  
Andrej Bohac ◽  
Cimen Karasu ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Diabetic Complications ◽  
Therapeutic Potential ◽  
Ex Vivo ◽  
Biological Activities ◽  
In Vivo Models ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Promising Therapeutic Approach

Aldose reductase (AR, ALR2), the first enzyme of the polyol pathway, is implicated in the pathophysiology of diabetic complications. Aldose reductase inhibitors (ARIs) thus present a promising therapeutic approach to treat a wide array of diabetic complications. Moreover, a therapeutic potential of ARIs in the treatment of chronic inflammation-related pathologies and several genetic metabolic disorders has been recently indicated. Substituted indoles are an interesting group of compounds with a plethora of biological activities. This article reviews a series of indole-based bifunctional aldose reductase inhibitors/antioxidants (ARIs/AOs) developed during recent years. Experimental results obtained in in vitro, ex vivo, and in vivo models of diabetic complications are presented. Structure–activity relationships with respect to carboxymethyl pharmacophore regioisomerization and core scaffold modification are discussed along with the criteria of ‘drug-likeness”. Novel promising structures of putative multifunctional ARIs/AOs are designed.

Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors

2005 ◽  
Vol 13 (2) ◽  
pp. 491-499 ◽  
Author(s):  
Federico Da Settimo ◽  
Giampaolo Primofiore ◽  
Concettina La Motta ◽  
Silvia Salerno ◽  
Ettore Novellino ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Derivatives Of

Permeability characteristics of novel aldose reductase inhibitors using rat jejunum in vitro

2006 ◽  
Vol 28 (1-2) ◽  
pp. 128-133 ◽  
Author(s):  
Katja Šturm ◽  
Lea Levstik ◽  
Vassilis J. Demopoulos ◽  
Albin Kristl
Keyword(s):  
Aldose Reductase ◽  
Rat Jejunum ◽  
Permeability Characteristics ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors
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