37428-90-3

Upstream product

• 141-84-4 2-thioxo-4-thiazolidinone 
• 555-16-8 4-nitrobenzaldehdye 
• 503-87-7 2-thiohydantoin 
• 2017-89-2 2-cyano-3-(4-nitrophenyl)-2-propenoic acid ethyl ester 

Downstream Products

• 129228-62-2 6-[1-(4-Nitro-phenyl)-meth-(Z)-ylidene]-2,3-dihydro-6H-imidazo[2,1-b]thiazol-5-one 
• 91121-97-0 2-Methylsulfanyl-5-[1-(4-nitro-phenyl)-meth-(Z)-ylidene]-3,5-dihydro-imidazol-4-one 

Relevant academic research and scientific papers

Chemoselective N-benzylation of 2-thiohydantoins and 2-thiobarbituric acids catalyzed by PEG-stabilized Ni nanoparticles and their anti-microbial activities

An efficient one pot chemoselective N-benzylation of 2-thiohydantoins and 2-thiobarbituric acids catalyzed by PEG-stabilized Ni nanoparticles has been reported, wherein the NH group of thiohydantoins and thiobarbituric acids is selectively benzylated and

Benzoxazolyl linked benzylidene based rhodanine and analogs as novel antidiabetic agents: synthesis, molecular docking, and in vitro studies

Benzoxazolyl linked meta- and para-substituted new chemical entities (5a–5h) featuring thiazolidinedione, rhodanine, hydantoin, and thiohydantoin moieties were synthesized and characterized by 1H NMR, 13C NMR, FT-IR, and HRMS spectra

Evaluation of michael-type acceptor reactivity of 5-benzylidenebarbiturates, 5-benzylidenerhodanines, and related heterocycles using NMR

Despite existing experimental and computational tools to assess the risk, the non-specific chemical modification of protein thiol groups remains a significant source of false-positive hits, particularly in academic drug discovery. Herein, we describe the

Bicyclic imidazole-4-one derivatives: A new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55

GPR18 and GPR55 are orphan G protein-coupled receptors (GPCRs) that interact with certain cannabinoid (CB) receptor ligands. In the present study bicyclic imidazole-4-one derivatives were discovered as new scaffolds for the development of antagonists for

AROMATIC IMIDAZOLIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASES OF BACTERIAL NATURE

The invention introduces new derivatives of aromatic imidazolidinones, which fall within the scope of the general formula I and their pharmaceutical forms of suitable additive salts with acids, wherein R1 and R2 are as defined herein

Privileged scaffolds or promiscuous binders: A comparative study on rhodanines and related heterocycles in medicinal chemistry

Rhodanines and related five-membered heterocycles with multiple heteroatoms have recently gained a reputation of being unselective compounds that appear as "frequent hitters" in screening campaigns and therefore have little value in drug discovery. However, this judgment appears to be based mostly on anecdotal evidence. Having identified various rhodanines and related compounds in screening campaigns, we decided to perform a systematic study on their promiscuity. An amount of 163 rhodanines, hydantoins, thiohydantoins, and thiazolidinediones were synthesized and tested against several targets. The compounds were also characterized with respect to aggregation and electrophilic reactivity, and the binding modes of rhodanines and related compounds in published X-ray cocrystal structures were analyzed. The results indicate that the exocyclic, double bonded sulfur atom in rhodanines and thiohydantoins, in addition to other structural features, offers a particularly high density of interaction sites for polar interactions and hydrogen bonds. This causes a promiscuous behavior at concentrations in the "screening range" but should not be regarded as a general knockout criterion that excludes such screening hits from further development. It is suggested that special criteria for target affinity and selectivity are applied to these classes of compounds and that their exceptional and potentially valuable biomolecular binding properties are consequently exploited in a useful way.

Synthesis and anti-inflammatory activity of new thiazolidine-2,4-diones, 4-thioxothiazolidinones and 2-thioxoimidazolidinones

New benzylidene imidazolidine and thiazolidine derivatives were prepared by nucleophilic addition on cyanoacrylates from substituted thioxoimidazolidinones, thiazolidinediones and thioxothiazolidinones. Anti-inflammatory activity of the synthesized thiazolidines was evaluated by the carrageenin-induced paw oedema test.

Glycine derivatives of imidazolones as potential ligands of glycine binding site of NMDA receptors. Part 1

The series of glycine derivatives of diphenyl or (un)substituted arylidene imidazolones was designed and obtained as potential ligands of the glycine binding site of NMDA receptors. The compounds were evaluated in vitro for their affinity to the glycine b