21262-23-7

Upstream product

• 105-39-5 chloroacetic acid ethyl ester 
• 3696-23-9 N-(4-chlorophenyl)thiourea 
• 79-11-8 chloroacetic acid 
• 3289-75-6 2-chloro-N-(4-chlorophenyl)acetamide 
• 106-47-8 4-chloro-aniline 
• 20949-66-0 2-methylsulfanyl-thiazol-4-one 
• 105-36-2 ethyl bromoacetate 
• 17356-08-0 thiourea 
• 1147550-11-5 ammonium thiocyanate 

Downstream Products

• 847021-33-4 2-(4-chloro-phenylimino)-7-phenyl-2,3-dihydro-thiazolo[4,5-d]pyrimidin-5-ol 
• 847021-39-0 2-(4-chloro-phenylimino)-7-(4-methoxy-phenyl)-2,3-dihydro-thiazolo[4,5-d]pyrimidin-5-ol 
• 847021-36-7 2-(4-chloro-phenylimino)-7-(4-hydroxy-phenyl)-2,3-dihydro-thiazolo[4,5-d]pyrimidin-5-ol 
• 847021-06-1 2-(2-{2-[(E)-4-Chloro-phenylimino]-4-oxo-5-[1-phenyl-meth-(Z)-ylidene]-thiazolidin-3-yl}-ethoxy)-isoindole-1,3-dione 
• 847021-15-2 2-(3-{2-[(E)-4-Chloro-phenylimino]-4-oxo-5-[1-phenyl-meth-(Z)-ylidene]-thiazolidin-3-yl}-propoxy)-isoindole-1,3-dione 
• 847021-24-3 2-(4-{2-[(E)-4-Chloro-phenylimino]-4-oxo-5-[1-phenyl-meth-(Z)-ylidene]-thiazolidin-3-yl}-butoxy)-isoindole-1,3-dione 
• 847021-09-4 2-(2-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-hydroxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-ethoxy)-isoindole-1,3-dione 
• 847021-12-9 2-(2-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-methoxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-ethoxy)-isoindole-1,3-dione 
• 847021-21-0 2-(3-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-methoxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-propoxy)-isoindole-1,3-dione 
• 847021-18-5 2-(3-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-hydroxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-propoxy)-isoindole-1,3-dione 
• 847021-27-6 2-(4-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-hydroxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-butoxy)-isoindole-1,3-dione 
• 847021-30-1 2-(4-{2-[(E)-4-Chloro-phenylimino]-5-[1-(4-methoxy-phenyl)-meth-(Z)-ylidene]-4-oxo-thiazolidin-3-yl}-butoxy)-isoindole-1,3-dione 
• 919364-90-2 2-(4-chlorophenylimino)-5-(4-fluoro-3-(trifluoromethyl)benzylidene)thiazolidin-4-one 
• 1394018-48-4 2-(4-chlorophenylimino)-5-((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thiazolidin-4-one 

Relevant academic research and scientific papers

SO2F2-Mediated N-Alkylation of Imino-Thiazolidinones

The N-alkylation of ambident and weakly nucleophilic imino-thiazolidinones has been developed via substitution with alkyl fluorosulfonates. These reactive electrophiles are obtained through the transformation of nontoxic, economic, and commercially availa

Design and microwave synthesis of new (5z) 5-arylidene-2-thioxo-1,3-thiazolinidin-4-one and (5z) 2-amino-5-arylidene-1,3-thiazol-4(5h)-one as new inhibitors of protein kinase dyrk1a

Here, we report on the synthesis of libraries of new 5-arylidene-2-thioxo-1,3-thiazolidin-4-ones 3 (twenty-two compounds) and new 2-amino-5-arylidene-1,3-thiazol-4(5H)-ones 5 (twenty-four compounds) with stereo controlled Z-geometry under microwave irradi

Novel compound bassed on thiazolidine and use thererof

The present invention relates to a novel compound and uses thereof. More specifically, the present invention provides: a novel compound based on thiazolidine which can effectively inhibit the aggregation of tau, one of the causes of Alzheimerandprime;s disease; and uses thereof. According to the novel compound and uses thereof composed as described above, it is possible to realize an effect of producing a therapeutic agent for Alzheimerandprime;s dementia due to tau aggregation.COPYRIGHT KIPO 2020

A Library of Thiazolidin-4-one Derivatives as Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitors: An Attempt To Discover Novel Antidiabetic Agents

Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin-4-one derivatives 8–22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5-(Furan-2-ylmethylene)-2-(4-nitrophenylimino)thiazolidin-4-one (17) exhibited potency with a competitive type of enzyme inhibition. structure–activity relationship studies revealed various structural facets important for the potency of these analogues. The findings revealed a requirement for a nitro group-including hydrophobic heteroaryl ring for PTP1B inhibition. Molecular docking studies afforded good correlation with experimental results. H-bonding and π–π interactions were responsible for optimal binding and effective stabilization of virtual protein-ligand complexes. Furthermore, in-silico pharmacokinetic properties of test compounds predicted their drug-like characteristics for potential oral use as antidiabetic agents.Additionally, a binding site model demonstrating crucial pharmacophoric characteristics influencing potency and binding affinity of inhibitors has been proposed, which can be employed in the design of future potential PTP1B inhibitors.

Synthesis of Novel Triazole Incorporated Thiazolone Motifs Having Promising Antityrosinase Activity through Green Nanocatalyst CuI-Fe3O4@SiO2 (TMS-EDTA)

In the present work, novel 5-((1-benzyl-1,2,3-triazol-4-yl)methoxybenzylidene)-2-(arylamino)thiazol-4-one thiazolone incorporated triazole derivatives have been designed as tyrosinase inhibitors. The compounds were synthesized through click reaction in good yield. Moreover, the antityrosinas activity of the synthesized derivatives was evaluated. In the search for establishing a click copper-catalyzed azide/alkyne cycloaddition (CuAAC) reaction under strict conditions, in terms of a novel air-stable, a recyclable and efficient magnetic catalyst was planned for new triazole derivatives as a well-organized copper iodide supported on the functionalized Fe3O4@SiO2 core-shell (CuI/Fe3O4@SiO2(TMS-EDTA) nanoparticles). The engineered nanocatalyst synthesized for the first time and characterized by different methods, including FT-IR spectroscopy, XRD, FESEM, EDX, TEM, TGA, and BET analysis. The excellent catalytic performance in ethanol with high surface area (351.7 m2g?1) and short reaction time for diverse functional groups (120–200 min), no use of toxic solvents, reusability of the catalyst, and using eco-friendly conditions are the advantageous of this work. Moreover,the nanocatalyst can be used at least five times without any significant decrease in the yield of the reaction. The thiazolidine-triazole derivatives 9a, 9c, 9e, and 9 g showed promising tyrosinase inhibitory activity with IC50 values in the range of 5.90–9.81 μM. The compounds were found to be considerably more potent tyrosinase inhibitors than the reference inhibitor kojic acid (IC50 = 18.36 μM).

Novel 2-(substituted phenyl Imino)-5-benzylidene-4-thiazolidinones as possible non-ulcerogenic tri-action drug candidates: synthesis, characterization, biological evaluation And docking studies

The present research was aimed at the synthesis and screening of 35 novel 2-(substituted phenyl imino)-5-benzylidene-4-thiazolidinones having different substitutions at imino phenyl and arylidene groups. The title compounds were synthesized by Knoevenagel

Design, synthesis and molecular docking studies of some thiazole clubbed heterocyclic compounds as possible anti-infective agents

The present work describes synthesis of a series of 5-((1-(4-(4-chlorophenyl)thiazol-2-yl)-3- aryl-1H-pyrazol-4-yl)methylene)-2-(arylimino)thiazolidin-4-one derivatives and their molecular docking and biological evaluation as possible antimalarial, anthelmintic and antimicrobial agents. The synthesis of compounds has been accomplished by adopting suitable synthetic methods. Structures of newly synthesized compounds were characterized and authenticated by spectral methods such as IR, 1H-NMR and mass spectra. Synthesized compounds were screened for their in vitro antimicrobial activity against selected bacterial strains and fungal strains viz. B. subtilis, S. aureus, E. coli, P. fluorescens, C. albicans, C. glabrata and antimalarial studies against P. falciparum. Titled compounds were also tested against Pheretima posthuma (earthworm) for their anthelmintic activity. Molecular docking was done to study the binding modes of the potent compounds against Escherichia coli (PDB ID: 1AB4) and Candida P450DM (PDB ID: 1EA1) enzymes. The results revealed that all the compounds exhibited moderate to significant antimicrobial activities. Antimalarial activity screening revealed that one compound 8i showed significant antimalarial activity with of IC50; 0.59 μg/mL as compared to standard drugs chloroquine (IC50= 0.020 μg/mL) and quinine (IC50; 0.268 μg/mL). The most active compound exhibited the mean paralysis time of 19.2 ± 0.9 min and mean death time of 31.7 ± 2.5 min. It can be concluded that some of the synthesized compounds have remarkable antiinfective, antimalarial and anthelmintic activity and are suitable candidates for further scientific exploration.

New thiazolidinyl analogs containing pyridine ring: Synthesis, biological evaluation and QSAR studies

A series of pyridine derivatives of thiazolidin-4-ones (4a-4o) has been synthesized. Structures of these compounds were established on the basis of elemental analysis, IR, 1H NMR, 13C NMR, and Mass spectral data. All the synthesized compounds have been evaluated for their anti-inflammatory and analgesic effects. The results showed that compound 2-[4-methylphenylimino]-5-(1H-pyridin-2-ylmethylidene)-1,3-thiazolidin-4-one (4d), 2-(2,4-dinitro-phenylhydrazinylidine)-5-(1H-pyridin-2-yl-methylidene)-1,3- thiazolidin-4-one (4h), and 2-[3-nitro-phenylimino]-5-(1H-pyridin-2-yl- methylidene)-1,3-thiazolidin-4-one (4j) exhibited good anti-inflammatory and analgesic activity. Compound 4h was found to be the most active compound of the series with an interesting dual anti-inflammatory and analgesic activity. Docking simulation was performed to position synthesized compounds into the active site of COX-2. The relationships of energy-based docking score with analgesic and anti-inflammatory activities were also investigated by linear regression method. The QSAR models with R 2 of 0.621 and 0.740 were developed for analgesic and anti-inflammatory activities, respectively.

Effect of chloro and fluoro groups on the antimicrobial activity of 2,5-disubstituted 4-thiazolidinones: A comparative study

The article reports the synthesis of a series comprising of twenty-one 2,5-disubstituted-4-thiazolidinone derivatives, bearing 3-chloro-4-fluorophenyl imino, 4-chlorophenyl imino and 3-chlorophenyl imino groups at position-2 and substituted arylidene grou

Synthesis and antimicrobial evaluation of some novel 2-(4- chlorophenylimino) thiazolidin-4-one derivatives

A series of 2-(4-chlorophenylimino)-5-((3-(p-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl) methylene) thiazolidin-4-one (3a-h) compounds were prepared from the 2-(4-chlorophenylimino) thiazolidin-4-one (1) and 1-phenyl-3-(p-substituted phenyl)-1H-pyrazole-4-carbaldehyde (2a-h). All compounds were characterized by elemental (C, H, N) analysis and spectral (FT-IR, 1H NMR and GC-MS) analysis. These newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial activity was observed and evaluated against the bacterial strains like Eschericha coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442) and against the fungal strains like Candida albicans (MTCC 227), Aspergillus niger (MTCC 282) and Aspergillus clavatus (MTCC 1323). All the synthesized compounds were found to possess moderate to excellent antimicrobial activity against above selected strains.