ChemInform Abstract: Synthesis of Pyrrolo(3,4-c)pyridine Derivatives Possessing an Acid Group and Their in vitro and in vivo Evaluation as Aldose Reductase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 27 (23) ◽  
pp. no-no
Author(s):  
A. DA SETTIMO ◽  
G. PRIMOFIORE ◽  
F. DA SETTIMO ◽  
F. SIMORINI ◽  
C. LA MOTTA ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Acid Group ◽  
Pyridine Derivatives ◽  
In Vivo Evaluation ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

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

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.

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 Isatin Derivatives as a New Class of Aldose Reductase Inhibitors With Antioxidant Activity

2021 ◽  
Author(s):  
Wenchao Liu ◽  
Huan Chen ◽  
Xiaonan Zhang ◽  
Xin Zhang ◽  
Long Xu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Acetic Acid ◽  
Aldose Reductase ◽  
Acid Group ◽  
Docking Studies ◽  
Side Chain ◽  
New Class ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Isatin Derivatives

Abstract In this work, isatin was employed as the scaffold to design aldose reductase inhibitors with antioxidant activity. Most of the isatin derivatives were proved to be excellent in the inhibition of aldose reductase (ALR2) with IC 50 values at submicromolar level, and (E)-2-(5-(4-methoxystyryl)-2,3-dioxoindolin-1-yl) acetic acid (9g) was identified as the most effective with an IC 50 value of 0.015 μM. Moreover, compounds 9a-h with styryl side chains at the C5 position of isatin showed potent antioxidant activity. Particularly, the phenolic compound 9h demonstrated similar antioxidant activity with the well-known antioxidant Trolox. Structure-activity relationship and molecular docking studies showed that the acetic acid group at N1 and C5 p-hydroxystyryl side chain were the key structures to increase the aldose reductase inhibitory activity and antioxidant activity.

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