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Design and Discovery of New Dual Carbonic Anhydrase IX and VEGFR-2 Inhibitors Based on the Benzenesulfonamide-Bearing 4-Thiazolidinones/2,4-Thiazolidinediones Scaffold.
Drug Dev Res
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Dual-targeting drug design has become a popular approach in investigating and developing potent anticancer agents. In this regard, carbonic anhydrase (CAIX) and vascular endothelial growth factor receptor (VEGFR-2) are emerging as highly effective targets in the battle against cancer. In the present study, two series of 4-thiazolidinones/2,4-thiazolidinediones carrying 2-methylbenzenesulfonamide derivatives were designed and synthesized as potential dual CAIX/VEGFR-2 inhibitors.
View Article and Find Full Text PDFSynthesis, Characterization, Antiglycation Evaluation, Molecular Docking, and ADMET Studies of 4-Thiazolidinone Derivatives.
ACS Omega
January 2024
Translational Bioinformatics Group, International Centre for Genetic Engineering and Biotechnology (ICGEB), Aruna Asaf Ali Marg 110067, New Delhi, India.
The design and development of new small-molecule glycation inhibitors are essential for preventing various chronic diseases, including diabetes mellitus, immunoinflammation, cardiovascular, and neurodegenerative diseases. 4-Thiazolidinone or thiazolidine-4-one is a well-known heterocyclic compound with the potential to inhibit the formation of advanced glycation end products. In the present work, we report the synthesis and characterization of four new 5-arylidene 3-cyclopropyl-2-(phenylimino)thiazolidin-4-one (-) compounds and their human serum albumin glycation inhibitory activity.
View Article and Find Full Text PDFSynthesis and Biological Evaluation of Novel 2-imino-4-thiazolidinones as Potential Antitumor Agents for Glioblastoma.
Med Chem
March 2022
Laboratório de Química Aplicada a Bioativos (LaQuiABio), Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas, Campus Universitário S/N, Capão do Leão, RS, Brazil.
Aims: The purpose of our study was to explore the molecular hybridization between 2- imino-4-thizolidione and piridinic scaffolds and its potential antitumor activity.
Background: Glioblastoma is the most aggressive glioma tumor clinically diagnosed malignant and highly recurrent primary brain tumor type. The standard of treatment for a glioblastoma is surgery, followed by radiation and chemotherapy using temozolomide.
In vitro evaluation of new 4-thiazolidinones on invasion and growth of Toxoplasma gondii.
Int J Parasitol Drugs Drug Resist
August 2021
Grupo GICOC, Universidad del Quindío, Armenia. Electronic address:
Treatments for toxoplasmosis such as pyrimethamine have shown numerous side effects. It has been reported that the likelihood of relapse associated with pyrimethamine-based therapy in patients with HIV and toxoplasmic encephalitis (TE) can have significant implications, even for patients who often develop new lesions in areas of the brain previously free of infection. This led us to research for new agents against Toxoplasma gondii.
View Article and Find Full Text PDFStructural design, synthesis and anti-Trypanosoma cruzi profile of the second generation of 4-thiazolidinones chlorine derivatives.
Chem Biol Interact
August 2021
Department of Pharmaceutical Sciences, Health Sciences Center, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil. Electronic address:
Chagas disease causes more deaths in the Americas than any other parasitic disease. Initially confined to the American continent, it is increasingly becoming a global health problem. In fact, it is considered to be an "exotic" disease in Europe, being virtually undiagnosed.
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