Aldose reductase and protein tyrosine phosphatase 1B inhibitors as a promising therapeutic approach for diabetes mellitus

A Kousaxidis, A Petrou, V Lavrentaki… - European Journal of …, 2020 - Elsevier
Diabetes mellitus is a metabolic disease characterized by high blood glucose levels and
usually associated with several chronic pathologies. Aldose reductase and protein tyrosine …

Design of improved antidiabetic drugs: a journey from single to multitarget Agents

VP Tassopoulou, A Tzara, AP Kourounakis - ChemMedChem, 2022 - Wiley Online Library
Multifactorial diseases exhibit a complex pathophysiology with several factors contributing to
their pathogenesis and development. Examples of such disorders are neurodegenerative …

The radical scavenging activity of 4-mercaptoimidazole: Theoretical insights into the mechanism, kinetics and solvent effects

QV Vo, NT Hoa, PC Nam, TQ Duong… - New Journal of …, 2023 - pubs.rsc.org
4-Mercaptoimidazole (4MC) is related to natural ovothiols known to be potent radical
scavengers. In spite of early reports of its good antioxidant activity, 4MC has attracted little …

Development of novel oxotriazinoindole inhibitors of aldose reductase: isosteric sulfur/oxygen replacement in the thioxotriazinoindole cemtirestat markedly improved …

M Hlavac, L Kovacikova, MS Prnova… - Journal of Medicinal …, 2019 - ACS Publications
Inhibition of aldose reductase (AR), the first enzyme of the polyol pathway, is a promising
approach in treatment of diabetic complications. We proceeded with optimization of the …

Development of novel indole-based bifunctional aldose reductase inhibitors/antioxidants as promising drugs for the treatment of diabetic complications

L Kovacikova, MS Prnova, M Majekova, A Bohac… - Molecules, 2021 - mdpi.com
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 …

Triglyceride-lowering effect of the aldose reductase inhibitor cemtirestat—another factor that may contribute to attenuation of symptoms of peripheral neuropathy in …

MS Prnova, L Kovacikova, K Svik, S Bezek… - Naunyn-Schmiedeberg's …, 2020 - Springer
Hyperglycemia is considered a key risk factor for development of diabetic complications
including neuropathy. There is strong scientific evidence showing a primary role of aldose …

3-Mercapto-5H-1,2,4-Triazino[5,6-b]Indole-5-Acetic Acid (Cemtirestat) Alleviates Symptoms of Peripheral Diabetic Neuropathy in Zucker Diabetic Fatty (ZDF) Rats: A …

M Soltesova Prnova, K Svik, S Bezek… - Neurochemical …, 2019 - Springer
Peripheral neuropathy is the most prevalent chronic complication of diabetes mellitus. Good
glycemic control can delay the appearance of neuropathic symptoms in diabetic patients but …

Protective effects of novel substituted triazinoindole inhibitors of aldose reductase and epalrestat in neuron-like PC12 cells and BV2 rodent microglial cells exposed to …

Z Elmazoglu, MS Prnova, M Stefek, AF Ceylan… - Neurotoxicity …, 2021 - Springer
Aldose reductase (AR) catalyzes the conversion of glucose to sorbitol in a NADPH-
dependent reaction, thereby increasing the production of reactive oxygen species (ROS) …

Antioxidant mechanisms in the neuroprotective action of cemtirestat: studies in chemical models, liposomes and rat brain cortical slices

MS Prnova, ON Medina-Campos, J Pedraza-Chaverri… - Neuroscience, 2020 - Elsevier
Neuroprotective action of the novel aldose reductase (AR) inhibitor cemtirestat (CMT), 2-(3-
thioxo-2H-[1, 2, 4] triazino [5, 6-b] indol-5 (3H)-yl) acetic acid, was recently proved in …

Oxidative degradation of high-molar-mass hyaluronan: Effects of some indole derivatives to hyaluronan decay

K Valachová, M Mach, L Šoltés - International Journal of Molecular …, 2020 - mdpi.com
Indole derivatives such as isatin (a natural compound), cemtirestat, stobadine, and its
derivatives (synthetic compounds) are known to have numerous positive effects on human …