We designed and synthesized a large number of novel thiazolidin-4-one derivatives for the evaluation of their anti-Toxoplasma gondii activity. This scaffold was functionalized at the N1-hydrazine portion with aliphatic, cycloaliphatic and (hetero)aromatic moieties. Then, a benzyl pendant was introduced at the lactamic NH of the core nucleus to evaluate the influence of this chemical modification on biological activity. The compounds were subjected to several in vitro assays to assess their anti-parasitic efficacy, cytotoxicity on fibroblasts, inhibition of tachyzoite invasion/attachment and replication after treatment. Results showed that fourteen of these thiazole-based compounds compare favorably to control compound trimethoprim in terms of parasite growth inhibition.
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http://dx.doi.org/10.1016/j.ejmech.2014.08.046 | DOI Listing |
Molecules
November 2024
Department of Chemistry, Faculty of Science, Sohag University, Sohag 82524, Egypt.
A series of new quinazolin-2,4-dione derivatives incorporating amide/eight-membered nitrogen-heterocycles -, in addition, acylthiourea/amide/dithiolan-4-one and/or phenylthiazolidin-4-one - and -. The starting compound was prepared by reaction of 4-(2,4-dioxo-1,4-dihydro-2-quinazolin-3-yl)-benzoyl chloride with ammonium thiocyanate and cyanoacetic acid hydrazide. The reaction of with strong electrophiles, namely, -aminophenol, -amino thiophenol, and/or -phenylene diamine, resulted in corresponding quinazolin-2,4-dione derivatives incorporating eight-membered nitrogen-heterocycles -.
View Article and Find Full Text PDFFuture Med Chem
December 2024
Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Institute, National Research Centre (NRC), Cairo, Egypt.
Aim: A new series of 3,4-dihydronaphthalen-1(2 h)-ylidene)hydrazineylidene)-5-substituted thiazolidin-4-one derivatives were designed and synthesized.
Results & Methodology: The new compounds were screened for in vitro antitumor activity against Hela cancer cell line. The compounds 7b, 7 h, and 7i produced more potent cytotoxicity than doxorubicin with IC values of 1.
Luminescence
December 2024
Department of Biochemistry, Institute of Chemistry, Faculty of Science, P. J. Šafárik University in Košice, Košice, Slovak Republic.
In this study, we employ spectroscopic, thermodynamic and molecular docking approaches to identify the mechanism by which thiazolidinone derivatives 4a-4d bind with human serum albumin. It has been suggested that the affinity of the interaction of derivatives 4a-4d with HSA is within the optimal range necessary for the transportation and distribution of compounds within the organism. The binding constant values for the derivative/HSA complexes were found to be 0.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Chair and Department of Organic Chemistry, Medical University of Lublin, 4A Chodzki Street, 20-093 Lublin, Poland.
ACS Omega
November 2024
Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahçeşehir University, Istanbul 34353, Türkiye.
Tryptamine, a monoamine alkaloid with an indole ring structure, is derived from the decarboxylation of the amino acid tryptophan, which is present in fungi, plants, and animals. Tryptamine analogues hold significant therapeutic potential due to their broad pharmacological activities, including roles as neurotransmitters and potential therapeutic agents for various diseases. Structural modifications of tryptamine enhance receptor selectivity and metabolic stability, improving therapeutic efficacy.
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