Search Results - "Maccari, Rosanna"
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Targeting Aldose Reductase for the Treatment of Diabetes Complications and Inflammatory Diseases: New Insights and Future Directions
Published in Journal of medicinal chemistry (12-03-2015)“…Aldose reductase (AR) is an aldo–keto reductase that has been widely investigated as an enzyme crucially involved in the pathogenesis of chronic complications…”
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Can Allostery Be a Key Strategy for Targeting PTP1B in Drug Discovery? A Lesson from Trodusquemine
Published in International journal of molecular sciences (01-06-2023)“…Protein tyrosine phosphatase 1B (PTP1B) is an enzyme crucially implicated in aberrations of various signaling pathways that underlie the development of…”
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In Search for Multi-Target Ligands as Potential Agents for Diabetes Mellitus and Its Complications-A Structure-Activity Relationship Study on Inhibitors of Aldose Reductase and Protein Tyrosine Phosphatase 1B
Published in Molecules (Basel, Switzerland) (10-01-2021)“…Diabetes mellitus (DM) is a complex disease which currently affects more than 460 million people and is one of the leading cause of death worldwide. Its…”
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In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…2-Thioxo-4-thiazolidinone derivatives were evaluated as aldose reductase inhibitors (ARIs) and most of them exhibited good or excellent in vitro efficacy. Out…”
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In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I
Published in Bioorganic & medicinal chemistry letters (01-09-2005)“…The characterization of two cyclooxygenase isoforms (COX), the rate-limiting enzyme for the synthesis of prostaglandins (PGs) from arachidonic acid, has…”
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Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives
Published in Bioorganic & medicinal chemistry (01-06-2008)“…In continuation of our studies, we here report a series of non-carboxylic acid containing 2,4-thiazolidinedione derivatives, analogues of previously…”
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Identification of new non-carboxylic acid containing inhibitors of aldose reductase
Published in Bioorganic & medicinal chemistry (01-06-2010)“…New non-carboxylic acid containing 5-arylidene-2,4-thiazolidinedione derivatives have been identified as aldose reductase inhibitors active at low micromolar…”
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Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones
Published in Bioorganic & medicinal chemistry letters (15-07-2007)“…A number of 5-arylidene-2,4-thiazolidinediones containing a hydroxy or a carboxymethoxy group in their 5-benzylidene moiety have been synthesised and evaluated…”
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5-Arylidene-4-thiazolidinone derivatives active as antidegenerative agents on human chondrocyte cultures
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-02-2013)“…5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by…”
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In Vitro Antimycobacterial Activities of 2′-Monosubstituted Isonicotinohydrazides and Their Cyanoborane Adducts
Published in Antimicrobial Agents and Chemotherapy (01-02-2002)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Modeling and biological evaluation of 3,3′-(1,2-ethanediyl)bis[2-(4-methoxyphenyl)-thiazolidin-4-one], a new synthetic cyclooxygenase-2 inhibitor
Published in European journal of pharmacology (12-07-2002)“…Within the series of chiral 3,3′-(1,2-ethanediyl)bis[2-arylthiazolidin-4-ones], the 3,4-dimethoxyphenyl substituted derivative was found in the primary…”
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Sodium-Glucose Cotransporter Inhibitors as Antidiabetic Drugs: Current Development and Future Perspectives
Published in Journal of medicinal chemistry (25-08-2022)“…Sodium-glucose cotransporter 2 (SGLT-2) inhibitors (gliflozins) represent the most recently approved class of oral antidiabetic drugs. SGLT-2 overexpression in…”
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Extending the investigation of 4-thiazolidinone derivatives as potential multi-target ligands of enzymes involved in diabetes mellitus and its long-term complications: A study with pancreatic α-amylase
Published in Carbohydrate research (01-01-2021)“…Diabetes mellitus is a multifactorial disease, which is frequently complicated by the development of hyperglycaemia-induced chronic complications. The therapy…”
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An investigation on 4-thiazolidinone derivatives as dual inhibitors of aldose reductase and protein tyrosine phosphatase 1B, in the search for potential agents for the treatment of type 2 diabetes mellitus and its complications
Published in Bioorganic & medicinal chemistry letters (15-12-2018)“…[Display omitted] •4-Thiazolidinones were synthesised and tested as dual AR/PTP1B inhibitors.•SAR, molecular docking and kinetic studies were carried out.•Two…”
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Protein-Tyrosine Phosphatase-1B Mediates Sleep Fragmentation-Induced Insulin Resistance and Visceral Adipose Tissue Inflammation in Mice
Published in Sleep (New York, N.Y.) (01-09-2017)“…Abstract Study Objectives Sleep fragmentation (SF) is highly prevalent and has emerged as an important contributing factor to obesity and metabolic syndrome…”
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Designed multiple ligands for the treatment of type 2 diabetes mellitus and its complications: Discovery of (5-arylidene-4-oxo-2-thioxothiazolidin-3-yl)alkanoic acids active as novel dual-targeted PTP1B/AKR1B1 inhibitors
Published in European journal of medicinal chemistry (05-04-2023)“…Type 2 diabetes mellitus (T2DM) is a serious chronic disease with an alarmingly growing worldwide prevalence. Current treatment of T2DM mainly relies on drug…”
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Structure–activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents
Published in European journal of medicinal chemistry (23-06-2014)“…A series of 5-(carbamoylmethoxy)benzylidene-2-oxo/thioxo-4-thiazolidinone derivatives (6–9) were synthesized as inhibitors of aldose reductase (AR), enzyme…”
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Low Molecular Weight Phosphotyrosine Protein Phosphatases as Emerging Targets for the Design of Novel Therapeutic Agents
Published in Journal of medicinal chemistry (12-01-2012)Get full text
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Discovery of 4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives active as novel potent allosteric inhibitors of protein tyrosine phosphatase 1B: In silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents
Published in European journal of medicinal chemistry (15-02-2017)“…New 4-{[5-arylidene-2-(4-fluorophenylimino)-4-oxothiazolidin-3-yl]methyl}benzoic acids (5) and 2-thioxo-4-thiazolidinone analogues (6) were synthesised as a…”
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Design and evaluation of non-carboxylate 5-arylidene-2-thioxo-4-imidazolidinones as novel non-competitive inhibitors of protein tyrosine phosphatase 1B
Published in Bioorganic chemistry (01-11-2019)“…[Display omitted] •5-arylidene-2-thioxo-4-imidazolidinones 7 are novel PTP1B allosteric inhibitors.•Most of compounds 7 proved to be interesting PTP1B…”
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