14016-49-0Relevant academic research and scientific papers
Synthesis, antioxidant and antimicrobial activities of novel thiopyrano[2,3-d]thiazoles based on aroylacrylic acids
Lozynskyi, Andrii,Zasidko, Viktoria,Atamanyuk, Dmytro,Kaminskyy, Danylo,Derkach, Halyna,Karpenko, Olexandr,Ogurtsov, Volodymyr,Kutsyk, Roman,Lesyk, Roman
, p. 427 - 436 (2017/05/29)
Abstract: Here it is described the synthesis, antioxidant and antimicrobial activity determination of novel rel-(5 R, 6 S, 7 R)-6-benzoyl-7-phenyl-2-oxo-3,5,6,7-tetrahydro-2H-thiopyrano[2,3-d]thiazole-5-carboxylic acids. The target compounds were obtained in good yields from 5-arylidene-4-thioxo-2-thiazolidinones and β -aroylacrylic acids via regio- and diastereoselective hetero-Diels–Alder reaction. The stereochemistry of the cycloaddition was confirmed by NMR spectra. The antioxidant and antimicrobial activity screening identified 7 compounds (3c, 3e, 3f, 3g, 3k, 3l, 3p) with a high level of free radical scavenging (43–77% DPPH assay), and compounds with significant influence on Staphylococcus aureus, Bacillus subtilis and Candida albicans (MIC 3.13–6.25 μ g/mL), but slight effect on Escherichia coli.
ANTAGONISTS OF THE THYROID-STIMULATING HORMONE RECEPTOR (TSHR)
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Page/Page column 39, (2017/12/09)
The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the trea
Synthesis, anticancer and antiviral activities of novel thiopyrano[2,3-d]thiazole-6-carbaldehydes
Lozynskyi, Andrii,Golota, Sergii,Zimenkovsky, Borys,Atamanyuk, Dmytro,Gzella, Andrzej,Lesyk, Roman
, p. 1245 - 1249 (2016/08/31)
Novel rel-(6R,7R)-2-oxo-7-phenyl-3,5,6,7-tetrahydro-2H-thiopyrano[2,3-d]thiazole-6-carbaldehydes were synthesized via regio- and diastereoselective hetero-Diels-Alder reaction of 5-arylidene-4-thioxo-2-thiazolidinones with acrolein. The synthesized compou
A simple green synthesis of (Z)-5-arylmethylene-4-thioxothiazolidines and thiopyrano[2,3-d]thiazolidine-2-thiones in PEG-400 under catalyst-free conditions
Metwally, Nadia Hanafy
, p. 528 - 537 (2014/08/18)
An improved Knoevenagel condensation of various aromatic aldehydes with thiazolidine-2,4-dithione and with 4-thioxothiazolidin-4-one can be achieved at room temperature in polyethylene glycol-400 without catalyst to afford (Z)-5-arylmethylene-4-thioxothia
Microwave-assisted synthesis, antimicrobial and cytotoxic activities of some 4-thioxo-thiazolidine-2-one derivatives
Alegaon, Shankar G.,Alagawadi, Kallanagouda R.
experimental part, p. 612 - 618 (2012/05/05)
A series of (Z)-5-arylidene-4-thioxo-thiazolidine-2-ones (4a-o) were synthesized using microwave irradiation technique. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR spectral studies and elemental analysis. All compounds were evaluated for their preliminary in vitro antimicrobial and cytotoxic activities. The investigation of antimicrobial activity profile revealed that compounds 4d, 4f, 4g, and 4h exhibited marked activity against S. aureus and E. faecalis as compared with the standard while compounds 4d and 4h exhibited good antifungal activities against C. albicans, A. flavus, A. niger and C. neoformans. In preliminary MTT cytotoxicity studies, the (Z)-5- arylidene-4-thioxo-thiazolidine-2-one derivatives (4k, 4l and 4m) were found most potent. Compound 4m inhibited proliferation of HeLa, HT29, A549 and MCF-7 cell lines with an IC50 values of 23, 22, 20 and 20 μM, respectively.
Synthesis and in vivo antidiabetic activity of novel dispiropyrrolidines through [3 + 2] cycloaddition reactions with thiazolidinedione and rhodanine derivatives
Murugan, Ramalingam,Anbazhagan,Sriman Narayanan
scheme or table, p. 3272 - 3279 (2009/10/17)
The synthesis of a series of novel dispiropyrrolidines has been accomplished by 1,3-dipolar cycloaddition reaction with 5-arylidene-1,3-thiazolidine-2,4-dione and 5-arylidene-4-thioxo-1,3-thiazolidine-2-one derivatives as dipolarophiles. The structure and stereochemistry of the cycloadduct have been established by single crystal X-ray structure and spectroscopic techniques. Molecular docking studies were performed on 1FM9 protein. The synthesized compounds were screened for their antidiabetic activity on male Wistar rats.
Substituted thio-arylidene thiazolidinones: synthesis and structural study
Albuquerque,Galdino,Chantegrel,Thomasson,Pitta,Luu-Duc
, p. 201 - 205 (2007/10/03)
The synthesis and physico-chemical properties of fourteen 4-thio-5-arylidene-thiazolidine-2-ones and eight 3-(4-bromophenacyl)-4-thio-5-arylidene-thiazolidine-2-ones are described. These products were synthetized by the aldolisation-crotonisation reaction between aromatic aldehydes and 4-thio-thiazolidine-2-one followed by N-alkylation of this substituted compounds.
