Syntheses of tolrestat analogs containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives

1991 ◽  
Vol 34 (8) ◽  
pp. 2504-2520 ◽  
Author(s):  
Jay Wrobel ◽  
Jane Millen ◽  
Janet Sredy ◽  
Arlene Dietrich ◽  
Beverly J. Gorham ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Orally Active ◽  
Fluoro Derivatives

Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat

1989 ◽  
Vol 32 (11) ◽  
pp. 2493-2500 ◽  
Author(s):  
Jay Wrobel ◽  
Jane Millen ◽  
Janet Sredy ◽  
Arlene Dietrich ◽  
Joseph M. Kelly ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Orally Active

Benzothiazol-2-ylcarboxylic acids with diverse spacers: A novel class of potent, orally active aldose reductase inhibitors

1997 ◽  
Vol 7 (13) ◽  
pp. 1677-1682 ◽  
Author(s):  
Tomoji Aotsuka ◽  
Naoki Abe ◽  
Kanako Fukushima ◽  
Naoki Ashizawa ◽  
Motoyuki Yoshida
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Orally Active

Potent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain

1992 ◽  
Vol 35 (3) ◽  
pp. 457-465 ◽  
Author(s):  
Banavara L. Mylari ◽  
Thomas A. Beyer ◽  
Pamela J. Scott ◽  
Charles E. Aldinger ◽  
Michael F. Dee ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Side Chain ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Orally Active

Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives

1992 ◽  
Vol 35 (12) ◽  
pp. 2155-2162 ◽  
Author(s):  
Banavara L. Mylari ◽  
William J. Zembrowski ◽  
Thomas A. Beyer ◽  
Charles E. Aldinger ◽  
Todd W. Siegel
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Orally Active

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.

Discovery of potential aldose reductase inhibitors using in silico docking studies

2012 ◽  
Vol 12 (2) ◽  
pp. 157-161 ◽  
Author(s):  
Arumugam Madeswaran ◽  
Muthuswamy Umamaheswari ◽  
Kuppusamy Asokkumar ◽  
Thirumalaisamy Sivashanmugam ◽  
Varadharajan Subhadradevi ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
In Silico ◽  
Docking Studies ◽  
In Silico Docking ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors
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