870554-59-9Relevant academic research and scientific papers
Synthesis and antidiabetic activity of morpholinothiazolyl-2,4- thiazolidindione derivatives
Ezer, Melis,Yildirim, Leyla Tatar,Bayro, Ornela,Verspohl, Eugen J.,Dundar, Oya Bozdag
, p. 419 - 427 (2012)
We report the synthesis and the in vitro insulin releasing and glucose uptake activity of the morpholino thiazolyl-2,4-thiazolidinediones (1-15). Compounds 5, 1115 (at lower concentration; 0.001mg/ml) were able to increase insulin release in the presence
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors
Caputo, Samantha,Di Martino, Simona,Cilibrasi, Vincenzo,Tardia, Piero,Mazzonna, Marco,Russo, Debora,Penna, Ilaria,Summa, Maria,Bertozzi, Sine Mandrup,Realini, Natalia,Margaroli, Natasha,Migliore, Marco,Ottonello, Giuliana,Liu, Min,Lansbury, Peter,Armirotti, Andrea,Bertorelli, Rosalia,Ray, Soumya S.,Skerlj, Renato,Scarpelli, Rita
, p. 15821 - 15851 (2020/12/23)
Acid ceramidase (AC) is a cysteine hydrolase that plays a crucial role in the metabolism of lysosomal ceramides, important members of the sphingolipid family, a diversified class of bioactive molecules that mediate many biological processes ranging from cell structural integrity, signaling, and cell proliferation to cell death. In the effort to expand the structural diversity of the existing collection of AC inhibitors, a novel class of substituted oxazol-2-one-3-carboxamides were designed and synthesized. Herein, we present the chemical optimization of our initial hits, 2-oxo-4-phenyl-N-(4-phenylbutyl)oxazole-3-carboxamide 8a and 2-oxo-5-phenyl-N-(4-phenylbutyl)oxazole-3-carboxamide 12a, which resulted in the identification of 5-[4-fluoro-2-(1-methyl-4-piperidyl)phenyl]-2-oxo-N-pentyl-oxazole-3-carboxamide 32b as a potent AC inhibitor with optimal physicochemical and metabolic properties, showing target engagement in human neuroblastoma SH-SY5Y cells and a desirable pharmacokinetic profile in mice, following intravenous and oral administration. 32b enriches the arsenal of promising lead compounds that may therefore act as useful pharmacological tools for investigating the potential therapeutic effects of AC inhibition in relevant sphingolipid-mediated disorders.
Synthesis and antimicrobial activity of some novel thiazolidine-2,4-dione derivatives
Mentese, Arzu,Ceylan-Uenluesoy, Meltem,Bozdag-Duendar, Oya,Altanlar, Nurten,Ertan, Rahmiye
scheme or table, p. 659 - 665 (2010/03/23)
In this study, a series of phenylethylsulfanyl-1,3-thiazolo-thiazolidine-2, 4-dione derivatives (VII a - f, VIIIa - f) and 5-methyl-[1,2,4]triazolyl- sulfanyl-1,3-thiazolo-thiazolidine-2,4-dione derivatives (IX a - f, Xa - f) were synthesized and evaluated for their antibacterial and antifungal activities against S. aureus (ATCC 25923), methicillin resistant S. aureus (MRSA ATCC 43300), B. subtilis (ATCC 6633), E. coli ( ATCC 23556) and C. albicans (ATCC10145). All the compounds were found active against used bacteria. ECV Editio Cantor Verlag.
Synthesis and pharmacological evaluation of some 3-phenacyl-5-benzylidene-thiazolidine-2,4-diones
De Lima,Perrissin,Chantegrel,Luu-Duc,Rousseau,Narcisse
, p. 831 - 834 (2007/10/02)
The synthesis of 54 3-phenacyl-5-benzylidene-thiazolidine-2,4-diones is reported. Eight of them were tested for anti-oedema, analgesic and anticonvulsant activity. Only one compound showed significant anti-oedematous and analgesic activity. Three compounds protected against tonic seizures and death.
