ChemInform Abstract: ALDOSE REDUCTASE INHIBITORS: A POTENTIAL NEW CLASS OF AGENTS FOR THE PHARMACOLOGICAL CONTROL OF CERTAIN DIABETIC COMPLICATIONS

1985 ◽  
Vol 16 (44) ◽  
Author(s):  
P. F. KADOR ◽  
J. H. KINOSHITA ◽  
N. E. SHARPLESS
Keyword(s):  
Aldose Reductase ◽  
Diabetic Complications ◽  
New Class ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Pharmacological Control

scholarly journals SYNTHESIS AND EVALUATION OF SOME NEW 2-(5-(4-BENZAMIDOBENZYLIDENE)-2,4DIOXOTHIAZOLIDIN-3-YL)ACETIC ACID ANALOGS AS ALDOSE REDUCTASE INHIBITORS

2016 ◽  
Vol 10 (1) ◽  
pp. 62
Author(s):  
Arun K. Gupta ◽  
Jyoti Pandey ◽  
Arshad Ali
Keyword(s):  
Diabetes Mellitus ◽  
Acetic Acid ◽  
Aldose Reductase ◽  
Significant Role ◽  
Diabetic Complications ◽  
New Class ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Excess Amount ◽  
Secondary Complication

ABSTRACTObjective: Aldose reductase (ALR) enzyme plays a significant role in conversion of excess amount of glucose into sorbitol in diabetic condition,inhibitors of which decrease the secondary complication of diabetes mellitus. Scarce treatment of diabetic complications has motivated our interestfor the search of new aldose reductase inhibitors (ARIs) endowed with more favorable biological properties.Methods: Newer (4-(benzamidobenzylidene)-2,4-dioxothiazolidin-3-yl) acetic acid derivatives were synthesized, and these compound wereevaluated for their ARI and antidiabetic activity.Results: ARI activity of synthesized compounds was found in the range of 57.8-71.9% at 5µg/mL. Similarly, synthesized compounds decrease bloodglucose level in the range of 64.4-70.5 mg/dl at 15 mg/kg body weight.Conclusion: (E)-2-(5-(4-(substituted benzamido)benzylidene)-2,4-dioxothiazolidin-3-yl)acetic acid analogs shows comparable ARI as well asantidiabetic activity. These new class of compounds might be address the diabetic complications with safety.Keywords: Aldose reductase inhibitors, Diabetes mellitus, N-acetic acid-2,4-thiazolidinediones. 

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.

Multifunctional aldose reductase inhibitors based on 2H-benzothiazine 1,1-dioxide

RSC Advances ◽  
2016 ◽  
Vol 6 (16) ◽  
pp. 12761-12769 ◽  
Author(s):  
Zhongfei Han ◽  
Xin Hao ◽  
Zehong Gao ◽  
Bing Ma ◽  
Changjin Zhu
Keyword(s):  
Aldose Reductase ◽  
Diabetic Complications ◽  
Drug Candidates ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

A series of benzothiazine derivatives were designed and synthesized for the development of drug candidates for diabetic complications.

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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